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Gallagher, Julie Marie. "The synthesis of 1-acetamido-2,6-anhydro-1,7-deoxy-L-glycero-L-galactitol (N-[β-L-fucopyranosylomethyl]-acetamide) and related derivatives." Scholarly Commons, 1989. https://scholarlycommons.pacific.edu/uop_etds/2182.
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One important goal of this thesis is the hydrogenation of the glycosyl cyanide, which has never been mentioned by any of the groups who have done work in this area, except for B. Coxon and G. Fletcher, who in 1964, reduced a tetra-O-acetyl-β-D-galactopyranosyl cyanide with lithium aluminum hydride. We were hoping to obtain, by reduction with hydrogen on Pd/C, an aminomethyl C-glycoside. It is believed that these aminomethyl C-glycosides are of potential biological importance especially in the area of AIDS and HIV therapy.
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Issac, Ibrahim Youhanna. "Studies in the lower temperature molten salts eutectics." Thesis, University of Southampton, 1989. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.252705.
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Marchand, Pascal. "Synthese et evaluation pharmacologique de derives indoliques a activites immunosuppressive et antitumorale (doctorat chimie therapeutique)." Nantes, 1999. http://www.theses.fr/1999NANT22VS.
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Zhang, Zichen. "Anticancer effects of hexamethylene bisacetamide on human colon carcinoma cells in vitro /." Hong Kong : University of Hong Kong, 1999. http://sunzi.lib.hku.hk/hkuto/record.jsp?B21021065.
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Lundell, Sandra J. "Quantum Mechanical Studies of N-H···N Hydrogen Bonding in Acetamide Derivatives and Amino Acids." DigitalCommons@USU, 2018. https://digitalcommons.usu.edu/etd/7309.
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Proteins are made of vast chains of amino acids that twist and fold into intricate designs. These structures are held in place by networks of noncovalent interactions. One of these, the hydrogen bond, forms bridges between adjacent pieces of the protein chain and is one of the most important contributors to the shape and stability of proteins. Hydrogen bonds come in all shapes and sizes and a full understanding of these not only aids in our understanding of proteins in general but can bridge the gap to finding cures to many protein-related diseases, such as sickle-cell anemia. The primary aim of this thesis is to discover if a specific type of hydrogen bond, the N-H···N bond, occurs within proteins and if so, if it contributes to the structure and stability of proteins.
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Borko, Matijević. "Građenje halogenidnih kompleksa kobalta(II) u rastopima smeše neorganskih soli i polarnih organskih jedinjenja." Phd thesis, Univerzitet u Novom Sadu, Prirodno-matematički fakultet u Novom Sadu, 2011. https://www.cris.uns.ac.rs/record.jsf?recordId=77320&source=NDLTD&language=en.
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U ovoj doktorskoj disertaciji proučavano je građenje kompleksa kobalta(II) sa hloridnim i bromidnim jonima u rastopima koji sadrže jednu neorgansku so i jedno organsko jedinjenje i/ili vodu pri različitom sastavu sistema i na različitim temperaturama. Jedan od sistema je amonijum-nitrat – acetamid – voda sastava NH4NO3∙(2,61-z)CH3CONH2∙zH2O (z = 0,0 1,61 i 2,61), a drugi sistem je amonijum–nitrat – dimetilsulfoksid (DMSO) sastava NH4NO3∙zDMSO (z = 1 – 6), na različitim temperaturama (35, 45, 55 i 65 oC). Cilj ovog istraživanja je bio određivanje stabilnosti kompleksa kobalta koji se grade sa sa halogenidnim jonima i komponentama rastvarača, pronalaženje kvalitativne i kvantitativne zavisnosti konstanti stabilnosti kompleksa kobalta(II) sa halogenidnim jonima od temperature i molskog odnosa komponenti sistema NH4NO3∙(2,61-z)CH3CONH2∙zH2O odnosno NH4NO3∙zDMSO, određivanje termodinamičkih parametara koji karakterišu reakcije asocijacije u ovim sistemima.In this dissertation the complex formation between cobalt(II) and halide ions in the melts consisting of one inorganic salt, an organic compound and/or water has been studied at different temperatures. Two molten salt systems have been investigated: 1) ammonium nitrate-acetamide-water system NH4NO3∙(2,61-z)CH3CONH2∙zH2O (z = 0.0 1.61 2.61) and 2) ammonium nitratedimethyl sulfoxide NH4NO3∙zDMSO (z = 1 – 6), at four different temperatures: 35, 45, 55 and 65 oC. The purpose of this work was to determine stability of cobalt(II) complexes formed with the halide ions and the components of the solvents, to discribe the qualitative and quantitative relationships between the stability of the complexes and the melt composition, as well as the changes in the cobalt(II) coordination due to a complex formation. Thermodynamic parameters for cobalt(II) – halide association process in these melts were alsodetermined.
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劉汝這 and Yue-huen Thomas Lau. "Ultrastructural and stereological investigation of the effects of hexamethylene bisacetamide on human colon carcinoma LoVo cells invitro." Thesis, The University of Hong Kong (Pokfulam, Hong Kong), 2000. http://hub.hku.hk/bib/B29872972.
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DRUOT, HOULLEMARE SOPHIE. "Influence des interactions homo- et heterochirales lors du dedoublement par cristallisation preferentielle de deux derives de l'alpha-methylbenzylamine : le n-acetamide et le chloroacetate." Caen, 1999. http://www.theses.fr/1999CAEN2029.
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Une etude comparative du dedoublement par cristallisation preferentielle classique et auto-ensemencee des derives chloroacetate et n-acetyl de l'-methylbenzylamine est realisee. Les resultats sont largement inferieurs aux maxima autorises par la thermodynamique. L'etude detaillee des diagrammes binaires revele l'existence de compose racemique instable dans le premier cas ou metastable pour le n-acetyl. Il est montre que les interactions heterochirales peuvent inhiber la croissance selective d'un enantiomere dans une solution quasi racemique. Dans le cas du chloroacetate, des experiences de re-croissance cristalline en solution aqueuse enantiomeriquement pure montrent de plus une totale dissymetrie de reconstruction des monocristaux liee a un effet de solvant.
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Meilhoc, Eliane. "Polyamines et differenciation induite par l'hexamethylene bis acetamide (hmba) de cellules erythroleucemiques de souris : role cle de la desacetylation de l'hmba dans cette differenciation." Clermont-Ferrand 2, 1986. http://www.theses.fr/1986CLF2D177.
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De nombreuses modifications membranaires, cytoplasmiques et nucleaires accompagnent ce processus de differenciation induite. La question fondamentale qui se pose est de savoir, lesquelles, parmi ces modifications sont necessaires a la differenciation des cellules de friend. Peu d'elements permettent d'y repondre actuellement. Nos travaux montrent que des changements dans le metabolisme des polyamines (baisse de l'activite de l'ornithine decarboxylase et des taux intracellulaires en putrescine et spermidine) sont necessaires a la differenciation induite des cellules de friend. Une ou plusieurs etapes dependantes de polyamines interviendraient tres tot dans le deroulement du processus de differenciation. Par ailleurs, les modifications du metabolisme des polyamines sont correlees avec l'accumulation des produits de desacetylation intracellulaire de l'hmba (n-acetyl-diamino-1,6-hexane et diamino-1,6-hexane)
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Conley, Matthew. "Supercritical Water Gasification of Two-Carbon Carboxylic Acid Derivatives." Ohio University / OhioLINK, 2018. http://rave.ohiolink.edu/etdc/view?acc_num=ohiou1542202432022198.
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Helayel, Michel Jos? Sales Abdalla. "O antagonismo com acetamida em experimentos com ovinos, caprinos e coelhos indica monofluoroacetato como princ?pio t?xico de Pseudocalymma elegans." Universidade Federal Rural do Rio de Janeiro, 2011. https://tede.ufrrj.br/jspui/handle/jspui/1206.
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Coordena??o de Aperfei?oamento de Pessoal de N?vel Superior - CAPES
This study aimed to evaluate the protective effect of acetamid in experimental poisoning by Pseudocalymma elegans in sheep, goats and rabbits, in order to prove indirectly that monofluoroacetate (MF) is responsible for the clinical signs and death of animals that ingested the plant. Experiments were performed to determine for sheep and goats the lethal dose of P. elegans collected in Rio Bonito, RJ, in different seasons, and to adjust the dose of acetamid to be administered. In the first experiment, four animals received 1.0g/kg of fresh P. elegans, and two others were pretreated with 2.0g/kg of acetamid. None of the animals showed clinical signs or died. Possibly, the plant could be less toxic, since it was collected at the end of the rainy season. In the second experiment, two sheep and two goats received 0.67 and 1.0g/kg of the dried plant, after pretreatment with 2.0 and 3.0g/kg of acetamid, respectively. All animals died, as the administered doses of P. elegans were very high. In the third experiment, two sheep and two goats received 0.333g/kg of dried P. elegans after previous administration of 2.0g/kg of acetamid; a week later, the protocol above was repeated, but without the antidote. In experiments with rabbits, doses of 0.5 and 1.0g/kg of dried P. elegans were given after administration of 3.0g/kg of acetamid; seven days later, the same protocol was repeated, except the administration of acetamide. This procedure, when acetamid was administered before, prevented the appearance of clinical signs and death of sheep, goats and rabbits. But the animals not treated with acetamid showed symptoms of poisoning and died. Clinically, the sheep and goats had tachycardia, engorged jugular vein, positive venous pulse, lateral recumbence, and muscle tremors. In the "dramatic phase?, the animals fell into lateral position, stretched the limbs, were paddling and died within minutes. The rabbits showed apathy, muscle tremors, vocalization and lateral decumbence minutes before death. At postmortem examination, the sheep and goats had engorged jugular veins and atria, dilated Vena cava cranialis and caudalis, as well as pulmonary edema, hepatic congestion and edema of the gallbladder subserosa. In rabbits, the main macroscopic alterations were dilated atria, engorged Vena cava cranialis and caudalis, and congested liver and diaphragm vessels. Histopathology revealed, in two sheep and one goat, vacuolar-hydropic degeneration of the distal convoluted kidney tubules, together with caryopicnosis. In the rabbits, the liver showed severe congestion with numerous shock corpuscles. The experimental results show indirectly that MF is to be held responsible for death of the animals that ingested P. elegans; since "acetate donor" compounds, such as acetamid, are capable to reduce the competitive inhibition of MF for the same active site (Coenzyme A) which prevents the formation of fluorocitrate, its active metabolite, formed in the body through the socalled "lethal synthesis".
O presente trabalho teve como objetivo avaliar o efeito protetor da acetamida nas intoxica??es experimentais por Pseudocalymma elegans (Bignoniaceae) em ovinos, caprinos e coelhos, com a finalidade de comprovar indiretamente que o monofluoroacetato ? respons?vel pela sintomatologia e morte dos animais que ingerem essa planta. Foram realizados experimentos para determinar a dose letal da planta coletada em Rio Bonito, RJ, em diferentes ?pocas do ano para ovinos e caprinos e ajustar a dose de acetamida a ser administrada. No primeiro experimento, dois ovinos e dois caprinos receberam 1,0 g/kg de P. elegans fresca e um animal de cada esp?cie foi tratado previamente com 2,0 g/kg de acetamida. Nenhum animal apresentou altera??es cl?nicas ou morreu. Ao que tudo indica a planta poderia estar menos t?xica, j? que foi coletada no fim da esta??o das ?guas. No segundo experimento, dois ovinos e dois caprinos receberam 0,67 e 1,0 g/kg da planta dessecada, ap?s tratamento pr?vio, com 2,0 e 3,0 g/kg de acetamida, respectivamente. Todos os animais morreram, pois administramos doses muito altas de P. elegans. No terceiro experimento, dois ovinos e dois caprinos receberam, 0,333 g/kg de P. elegans dessecada, ap?s administra??o pr?via de 2,0 g/kg de acetamida. Uma semana depois, o protocolo acima foi repetido, por?m sem o ant?doto. Nos experimentos com coelhos, foram administradas doses de 0,5 e 1,0 g/kg de P. elegans dessecada ap?s a administra??o de 3,0 g/kg de acetamida. Sete dias depois, o mesmo protocolo foi repetido, com exce??o da administra??o de acetamida. Esta, quando administrada previamente, evitou o aparecimento dos sinais cl?nicos e a morte dos ovinos, caprinos e coelhos, j? os animais n?o tratados com acetamida apresentaram sintomatologia e morreram. Clinicamente, os ovinos e caprinos manifestaram taquicardia, jugulares ingurgitadas, pulso venoso positivo, dec?bito esternal e tremores musculares. Na ?fase dram?tica?, os animais ca?am em dec?bito lateral, esticavam os membros, faziam movimentos de pedalagem e morriam em poucos minutos. Nos coelhos observaram-se apatia, tremores musculares, dec?bito lateral e vocaliza??o minutos antes da morte. A avalia??o macrosc?pica revelou, nos ovinos e caprinos, jugulares ingurgitadas, aur?culas, veia cava caudal e cranial dilatadas, al?m de edema pulmonar, congest?o hep?tica e edema na subserosa da ves?cula biliar. Nos coelhos as principais altera??es observadas foram aur?culas dilatadas, veia cava caudal e cranial ingurgitadas, f?gado e vasos do diafragma congestos. O exame histopatol?gico revelou, em dois ovinos e um caprino, degenera??o hidr?pico-vacuolar dos t?bulos urin?feros contornados distais associada ? cariopicnose. Nos coelhos havia congest?o hep?tica acentuada com numerosos corp?sculos de choque. Nossos resultados comprovam, de forma indireta, que o MF ? respons?vel pela morte dos animais que ingerem essa planta, uma vez que compostos ?doadores de acetato? como a acetamida, s?o capazes de reduzir a inibi??o competitiva do MF pelo mesmo s?tio ativo (Coenzima A), o que impede a forma??o do fluorocitrato, seu metab?lito ativo, formado no organismo por meio da denominada ?s?ntese letal?.
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Oliveira, Sara Barone de. "Desenvolvimento de métodos bioanalíticos para acetamida." Master's thesis, Universidade de Aveiro, 2011. http://hdl.handle.net/10773/8076.
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Mestrado em QuímicaO presente trabalho teve como objectivo desenvolver um método bioanalítico baseado em sensores acústicos, para detectar e quantificar amidas tóxicas, entre as quais acetamida e acrilamida. Utilizou-se a enzima amidase (EC 3.5.1.4) de Pseudomonas aeruginosa L10, para converter a acetamida em compostos de menor toxicidade como o ião amónio e ácido acético. O ião amónio foi detectado por um sensor acústico com um revestimento químico apropriado. Testaram-se dois sistemas associando as duas componentes (química e biológica). No primeiro depositaram-se as duas componentes sobre um cristal. No segundo, inseriu-se num sistema de injecção em iluxo (FIA) o cristal revestido com o componente químico e a biológico foi imobilizado num biorreactor. Na concepção do biorreactor, testaram-se vários métodos de imobilização para o biocatalisador. Este foi confinado em contas de alginato de cálcio e imobilizado em esferas e capilares de vidro silanizados. A silanização foi feita pelo método de sol-gel e com solventes orgânicos com 3-aminopropiltrietoxissilano (APTS). A imobilização do biocatalisador foi feita com glutaraldeído (GA). Em todos estes casos, obtiveram-se respostas da conversão da acetamida pela amidase, tendo-se conseguido melhores resultados com a funcionalização das paredes do capilar com extracto celular.
The aim of this work was to develop a bioanalytical method based on an acoustic sensor to detect and quantify toxic amides namely acetamide and acrylamide. The enzyme amidase (EC 3.5.1.4) from Pseudomonas aeruginosa L10 was used to convert acetamide in less toxic compounds such as ammonium ion and acetic acid. The ammonium ion was detected by an acoustic sensor with an appropriate chemical coating. Two systems combining a chemical sensitive coating and a biocatalyst were tested. One of them was a two layer acoustic sensor, while the other includes a bioreactor separated from the chemical sensor. The last one, is part of a flow injection analytical system (FIA). For the design of the bioreactor, several immobilization methods were tested. Biocatalyst was present in whole cells of Pseudomonas aeruginosa L10 or cellular extract. The biocatalyst was either confined in calcium alginate beads or immobilized in silanized glass capillaries and glass beads. The silanization was based on the sol-gel techniques and reaction with organic solvents using 3-aminopropyltriethoxysilane (APTS). The biocatalyst was immobilized with gluraldehyde (GA). In all the experiments responses from conversion of acetamide mediated by the amidase were obtained. The best results were achieved with the functionalization of the capillary walls with celular extract.
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Zink, Landon. "Synthesis of N-(substituted phenyl) acetamides." Digital Commons @ East Tennessee State University, 2011. https://dc.etsu.edu/honors/131.
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Barrandon, Charlotte. "L' échange dynamique de l'ARN 7SK entre le facteur de transcription P-TEFb et les hnRNP." Paris 6, 2007. http://www.theses.fr/2007PA066181.
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L’ARN 7SK est devenu un paradigme d'ARN non codants régulateurs de la transcription. Les années précédentes, notre laboratoire a montré qu’il s’associe à la protéine HEXIM1 et au facteur de transcription P-TEFb (Positive Transcription Elongation Factor b) au sein d’un même complexe. Il en résulte une inactivation du P-TEFb. Ces interactions sont dynamiques, elles sont en perpétuelle formation/dissociation. Des traitements qui inhibent la transcription entraînent la séparation de l’ARN 7SK et du P-TEFb ce qui provoque une accumulation de la forme active de ce dernier. L’ARN 7SK libéré n’est pas dégradé mais s’intègre à d’autres snRNP7SK que nous avons caractérisées. Grâce à une purification des snRNP7SK, nous avons identifié des composants de ces 7SK snRNP : hnRNPQ/R et hnRNPA. Lors d’une inhibition transcriptionnelle, la liaison de l’ARN 7SK à ces hnRNPs augmente. Par ailleurs, l’absence de ces protéines perturbe la dissociation du P-TEFb. Ces protéines sont donc indispensables à l’équilibre dynamique du P-TEFb. Ces hnRNP sont déjà connues pour être engagées dans la maturation des ARN pré-messagers. Cette observation constitue une nouvelle illustration du couplage existant entre transcription et maturation des pré-messagers.
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Abban, Grace. "Methodology Study of N-deacetylation of 4-acetamido-perfluoroalkylbenzenesulfonimide." Digital Commons @ East Tennessee State University, 2015. https://dc.etsu.edu/etd/2553.
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In order to improve the synthetic route for diazonium perfluoroalkyl benzenesulfonylimide (PFSI) zwitterionic monomers, N-deacetylation of the coupling product was proposed to replace the reduction of aromatic amine intermediates. A series of hydrolysis methods, such as acid and base catalyzed refluxing, were explored for the N-deacetylation to obtain the PFSI aromatic amine. Factors such as temperature, concentration of acid/base and the time needed for the reaction to take place were investigated in an attempt to optimize the reaction condition. The basic hydrolysis was preferred since it was expected to carry out the N-deacetylation and debromination in one batch reaction. N-deacetylation in base at high concentrations was successful, however, side reaction of the perfluorovinyl ether occurred. It was discovered that the best N-deacetylation method is to reflux/sonicate the coupling product with acid in methanol for six hours. The intermediates and purified products were characterized with 1HNMR, 19FNMR, GC-MS and IR.
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Wardle, Nicholas James. "Synthesis and characterisation of novel 1-acetamido-2,2-biscarbamyl-ethanephosphonate derivatives." Thesis, London Metropolitan University, 1998. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.287630.
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Sierra, Sánchez Ana Gabriela. "TRATAMIENTO DEL N-(4-hidroxifenil) acetamida EN SOLUCIÓN ACUOSA MEDIANTE FOTOELECTROXIDACIÓN CON UNA CONFIGURACIÓN DDB-Fe Y DDB-Cu." Tesis de Licenciatura, Universidad Autónoma del Estado de México, 2018. http://hdl.handle.net/20.500.11799/94929.
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La presencia en el medio de nuevos compuestos xenobióticos es una consecuencia del uso de productos químicos en diferentes campos productivos y en la vida cotidiana. Los fármacos y productos de cuidado personal (FPCP) son ejemplo de ellos y hacen referencia a cualquier producto utilizado para la salud personal, con fines cosméticos o empleados por la agroindustria para promover el crecimiento o la salud del ganado. Cantidades importantes de estos productos se utilizan anualmente alrededor del mundo, y en concentraciones muy pequeñas algunos FPCP pueden causar la alteración en el sistema endocrino y afectar el desarrollo de los organismos acuáticos y la vida silvestre (Lintelmann et al., 2003).En el presente trabajo de investigación se llevó a cabo el tratamiento del N-(4-hidroxifenil) acetamida en solución acuosa mediante electroxidación y fotoelectroxidación. Para ello, se empleó una celda electroquímica en donde el tratamiento de soluciones acuosas de acetaminofén (ACT) a diferentes concentraciones dio lugar. Se planteó un diseño factorial 23, analizando las variables de: intensidad de corriente (0.5 y 1.0 A), configuración electródica (DDB-Fe y DDB-Cu) y presencia o ausencia de luz UV. Se prepararon soluciones de acetaminofén de 10, 50 y 80 mg L-1. La caracterización de las soluciones acuosas antes y después del tratamiento se realizó mediante FT-IR, UV-Vis, DQO, DBO5, COT, CT y Fluorescencia. Con los resultados obtenidos de las ocho corridas del diseño 23 empleando la concentración más alta de ACT (80 mg L-1), se determinaron las condiciones óptimas de operación, las cuales fueron: 1.0 A, configuración DDB-Fe y presencia de luz UV; bajo estas condiciones se obtuvo una remoción del 82.75 % de COT. Esto sustentado con la estimación del efecto calculado mediante el algoritmo de Yates. El electrolito soporte fue NaCl (2.5 g L-1) y el pH inicial de 5.5; el tiempo de tratamiento de 3 h y los tiempos de monitoreo de 5, 10, 15, 30, 45, 60, 90, 120, 150 y 180 minutos. Las concentraciones de 50 y 10 mg L-1 se trataron mediante fotoelectroxidación, empleando una lámpara UV de onda corta (254 nm) y en las condiciones óptimas de operación previamente descritas, se obtuvo una mineralización de 77.16 % y 50.29 % de COT, respectivamente. Finalmente se realizó el estudio cinético para la oxidación del N-(4-hidroxifenil) acetamida, se determinaron las constantes cinéticas y el tiempo de vida media en presencia y ausencia de luz UV (k= 3.66 x 10-2 min-1, t1/2= 18.934 min; k= 2.66 x 10-2 min-1, t1/2= 25.956 min, respectivamente); así como el posible mecanismo de degradación del mismo.
SIEA. El presente trabajo se realizó en el Centro Interamericano de Recursos del Agua (CIRA), a través del proyecto 4482/2018/CI, UAEMéx.
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MENCIU, CECILIA CEZARINA. "(indol-3-yl)acetamides et analogues structuraux a activites antiallergique, immunomodulatrices et antitumorales." Nantes, 1997. http://www.theses.fr/1997NANT2018.
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Divers (indol-3-yl)acetamides et 2-(indol-3-yl)ethylamines substitues en 1, sur l'homocycle et sur la chaine amidique, ont ete synthetises. La pharmacomodulation, visant a exalter des activites antiallergique et/ou antitumorales, a notamment conduit a : -des enchainements glyoxamide, hydroxyacetamide, -des derives tricycliques issus de la 5,6-dihydro-4h-pyrrolo3,2,1-i,jquinoleine, du 9h-pyrido3,4-bindole. La determination du potentiel antiallergique a ete realisee par mise en oeuvre des tests d'inhibition de la liberation d'histamine et de la production des interleukines 4 et 5. La mis en evidence des proprietes immunomodulatrice a ete determinee par exploitation des tests d'inhibition de l'interleukine 2 et d'inhibition de la peptidyl-prolyl-cis, trans -isomerase. Enfin, l'activite antitumorale de ses composes a ete evaluee in vitro sur divers lignees cellulaires (celleules kr, l 1210, lncap et sk-ov-3) en exploitant le test xtt, estimant l'activite mitochondriale. Cette etude a permis de selectionner des molecules actives, dans ces divers domaines, qui font actuellement l'objet d'investigations complementaires.
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Kannengießer, Raphaela [Verfasser], Wolfgang [Akademischer Betreuer] Stahl, and Arne [Akademischer Betreuer] Lüchow. "Structures and dynamics of formamides, acetamides, and propionamides / Raphaela Kannengießer ; Wolfgang Stahl, Arne Lüchow." Aachen : Universitätsbibliothek der RWTH Aachen, 2017. http://d-nb.info/116141178X/34.
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Contini, A. "Synthesis, in silico and pharmacological evaluation of 2-pyridin-acetamides as tyrosine kinase inhibitors." Doctoral thesis, Università degli Studi di Milano, 2003. http://hdl.handle.net/2434/174341.
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A new synthesis of 2-pyridineacetamides was developed starting from pyran-2-one N-functionalized amidines.
Secondary amines reacted in a sealed tube with the above-mentioned amidines and, by nucleophilic attack on
pyran-2-one nucleus and thermal rearrangement, afforded exclusively the desired 2-pyridineacetamide derivatives.
Such compounds have been pharmacologically tested on smooth muscular cells proliferation and resulted active
with an IC50 ranging from 40 to 0.7 µM. With the aid of molecular modeling tools a potential mechanism of action
has been proposed. The pharmacological activity seems to be due to tyrosine kinase receptors inhibition.
In silico experiments shows a notable selectivity toward the epidermal derived growth factor receptor kinase (EGFRK)
and the platelet derived growth factor receptor kinase (PDGFRK) if compared with the vascular endothelial
derived growth factor receptor kinase (VEGFRK) and the fibroblast derived growth factor receptor kinase (FGFRK).
The predicted potency of the 2-pyridineacetamides described in the present study is comparable to that of known
EGFRK inhibitor TarcevaTM. Preliminary pharmacological experiments conducted on rat's aorta smooth muscular cells
confirm the observed computational results.
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Peixoto, Isabelle Nogueira. "Estudos químicos de derivados mesoiônicos do sistema 1,3- Tiazólio-5-tiolato com acetamidas substituídas e suas Potencialidades antifúngicas contra cepas de candida Albicans." Universidade Federal da Paraíba, 2016. http://tede.biblioteca.ufpb.br:8080/handle/tede/9002.
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This work describes the synthesis, characterization and antifungal potential of twelve mesoionic derivatives from the 1,3-thiazolium-5-thiolate system. The compounds, totally unprecedented, were divided in two classes: one class derived from the mesoionic 2-(4-chlorophenyl)-3-methyl-4-(4-isopropylphenyl)-1,3-thyazolium-5- thiolate with ten substituted acetamides and other class derived from the mesoionic 2- (4-chlorophenyl)-3-methyl-4-(4-methylphenyl)-1,3-thyazolium-5-thiolate also with ten substituted acetamides. This compounds synthesis, which presented satisfactory yields (85 to 95 %), occurred in four stages: first the intermediary N-methyl-Carylglicine was synthesized via Strecker reaction with p-substituted aldehydes, followed by its aroylation to obtain N-methyl-N-aroyl-C-arylglicine, the next step was its cyclodehydration with acetic anhydride, 1,3-dipolar cycloaddition and cyclorevertion induced by CS2 to obtain the mesoionic compounds from the 1,3- thiazolium-5-thyolate as free base. Lastly, the mesoionic compounds were converted into his respective salts by the treatment with ten substituted acetamides. All compounds were characterized by spectroscopic techniques IR, NMR 1H and NMR 13C, and their antifungal potential against five strains of Candida albicans were evaluated. Only four compounds exhibited efficient activity (MI-1-A3, MI-1-A4, MI- 1-A6 and MI-1-A7) with MIC between 256 – 512 μg mL-1. An in silico investigation of the mesoionic compounds, the substituted acetamides and the mesoionic derivatives was also made and the results showed that both mesoionic compounds and his derivatives are good candidates to be a drug while all substituted acetamides should present high toxicity.
Neste trabalho descreve-se a síntese, caracterização e potencial antifúngico de vinte derivados mesoiônicos do sistema 1,3-tiazólio-5-tiolato. Os compostos, inéditos, foram divididos em duas classes: uma classe de compostos derivados do mesoiônico 2-(4-clorofenil)-3-metil-4-(4-isopropilfenil)-1,3-tiazólio-5-tiolato com dez acetamidas substituídas e outra classe de compostos derivados do mesoiônico 2-(4-clorofenil)-3- metil-4-(4-metilfenil)-1,3-tiazólio-5-tiolato e também com dez acetamidas substituídas. A síntese desses compostos, que apresentou rendimentos satisfatórios (85 a 95 %), ocorreu em quatro etapas: primeiramente o intermediário N-metil-Carilglicina foi sintetizado via reação de Strecker com aldeídos p-substituídos, seguido de sua aroilação para obter o N-metil-N-aroil-C-arilglicina, seguida da ciclo desidratação com anidrido acético, cicloadição e cicloreversão 1,3-dipolar induzida por CS2 para obter os mesoiônicos do sistema 1,3-tiazólio-5-tiolato na forma de base livre. Por fim os mesoiônicos foram convertidos em seus respectivos sais através do tratamento com dez acetamidas substituídas. Todos os compostos, intermediários, mesoiônicos, acetamidas e derivados mesoiônicos, foram caracterizados por técnicas espectroscópicas de IV, RMN de 1H e 13C e avaliou-se o potencial antifúngico dos derivados mesoiônicos contra cinco cepas de Candida albicans. Dentre os vinte derivados mesoiônicos investigados, apenas quatro, MI-1-A3, MI-1-A4, MI-1-A6 e MI-1-A7, exibiram eficiente atividade com concentrações inibitórias mínimas entre 256 – 512 μg mL-1. Neste trabalho realizou-se ainda uma investigação in silico dos compostos mesoiônicos, das acetamidas substituídas e dos derivados mesoiônicos e os resultados indicaram que tanto os compostos mesoiônicos quanto seus derivados são bons candidatos a fármacos enquanto que as dez acetamidas substituídas investigadas devem apresentar elevada toxicidade.
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Dupont, Jairton. "Activation-fonctionnalisation intramoleculaire de liaisons c-h par le palladium." Université Louis Pasteur (Strasbourg) (1971-2008), 1988. http://www.theses.fr/1988STR13197.
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Bu, Qingqing. "Ruthenium- and Cobalt-Catalyzed C-H Activation." Doctoral thesis, Niedersächsische Staats- und Universitätsbibliothek Göttingen, 2018. http://hdl.handle.net/11858/00-1735-0000-002E-E4FC-F.
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Piva, Luíza Cesca. "Uso do gene amdS (acetamidase) como marca de seleção dominante em Pichia pastoris." reponame:Repositório Institucional da UnB, 2015. http://dx.doi.org/10.26512/2015.02.D.17857.
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Dissertação (mestrado)—Universidade de Brasília, Instituto de Ciências Biológicas, Departamento de Biologia Celular, Programa de Pós-graduação em Biologia Molecular, 2015.Submitted by Aline Girardi (alinegirardiunb@gmail.com) on 2015-04-01T19:26:55Z No. of bitstreams: 1 2015_LuízaCescaPiva.pdf: 2317519 bytes, checksum: 29251421288ca0cf8f14fde7573ec0cb (MD5)
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A levedura Pichia pastoris tem sido bastante explorada na produção de proteínas heterólogas, graças a algumas vantagens apresentadas por esse sistema, tais como: técnicas de manipulação genética disponíveis, crescimento em altas densidades celulares, realização de modificações pós-traducionais e secreção eficiente de proteínas. Contudo, esse sistema ainda possui algumas limitações no que se refere às ferramentas de genética molecular. Por exemplo, para que diversas modificações sejam introduzidas na mesma linhagem, faz-se necessário o uso de múltiplas marcas de seleção ou de estratégias que permitam a sua reutilização. Em Pichia, o uso de marcas recicláveis ainda é limitado. Nesse contexto, destaca-se o gene amdS (acetamidase) de Aspergillus nidulans, que permite a seleção de fungos em meio de cultura contendo acetamida como única fonte de nitrogênio e a contrasseleção em meio contendo a droga fluoroacetamida. Em conjunto com a contrasseleção do gene amdS, o sistema Cre-loxP de recombinação sítio-específica pode ser utilizado para facilitar a excisão da marca de seleção. Neste trabalho, o uso da marca amdS foi testado em P. pastoris e, como prova de conceito, foi feita a deleção do gene ADE2, uma carboxilase envolvida na síntese “de novo” de purinas. Primeiramente, uma ORF endógena que codifica para uma amidase putativa foi deletada. Em seguida, foi construído um vetor contendo um cassete com o gene amdS flanqueado por sítios loxP além do gene repórter EGFP para testar a eficiência da marca em P. pastoris. A construção amdS-loxP foi também utilizada em cassetes de deleção para os genes ADE2 e URA5. Após a deleção do gene ADE2, um plasmídeo replicativo contendo o gene da recombinase CreA (pYRCre2) foi utilizado para a excisão da marca, para permitir a reutilização do gene amdS em outros eventos de deleção. A integração do vetor contendo o gene amdS mostrou que esta nova marca de seleção é aplicável em P. pastoris com a vantagem de permitir a contrasseleção de transformantes após o uso do sistema de recombinação Cre-loxP. Esta nova ferramenta traz alternativas na manipulação genética da levedura reduzindo problemas como a necessidade de expressão de diversas marcas dominantes.
The yeast Pichia pastoris has been widely explored for the production of heterologous proteins due to certain advantages presented by this system, such as: molecular genetic techniques available, growth at high cell densities, post-translational modifications and efficient protein secretion. However, this system still has some limitations related to the tools used for genetic modifications. For example, in order for many genetic modifications to be done in the same strain, one needs to use multiple selection marks or strategies that allow marker reusing. In Pichia, the use of recyclable markers is still limited. The amdS gene from Aspergillus nidulans stands out in this context because it allows the selection of fungi in medium that contains acetamide as sole nitrogen source, as well as the counterselection in medium that contains the drug fluoroacetamide. Along with the counterselection property of the amdS gene, the Cre-loxP site-specific recombination system can be used to help in selection marker excision. In this work, the amdS selection mark was tested in P. pastoris and, as proof of concept, the ADE2 gene coding for a carboxylase involved in purine synthesis was deleted. Firstly, an endogenous ORF coding for a putative amidase was deleted. Subsequently, a vector containing a cassette with the amdS gene flanked by loxP sites and a EGFP gene was constructed in order to test the selection marker in P. pastoris. The amdS-loxP construction was also used in deletion cassettes for ADE2 and URA5 genes. After the ADE2 gene deletion, a replicative plasmid containing the CreA recombinase gene (pYRCre2) was used for marker excision, allowing the use of the amdS gene in further gene deletion events. Integration of the vector containing the amdS gene showed that this new selection marker is applicable in P. pastoris with the advantage of allowing counterselection after using the Cre-loxP recombination system. This new tool brings an alternative for P. pastoris genetic manipulation, reducing problems such as the expression of many dominant selection markers simultaneously.
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Wolf, Lucas. "Síntese de heterociclos: 2-alquil/arilcalcogeno-n-(4-aril-1,3-tiazol-2-il)acetamidas e (s)-n-(1-(3-aril-1,2,4-oxadiazol-5-il)alquil)-2-(calcogenofenil) acetamidas derivados de organocalcogênios." Universidade Federal de Santa Maria, 2015. http://repositorio.ufsm.br/handle/1/4271.
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Coordenação de Aperfeiçoamento de Pessoal de Nível SuperiorIn the present work, a series of 2-alkyl/arylchalcogenide-N-(4-aryl-1,3-thiazol-2-yl)acetamide was prepared via addition of aryl or alkyl chalcogenides. This methodology allowed the preparation of new derivatives of 2-amino-1,3-thiazoles in good yields. The compound synthesized is intended to evaluate the biological potential from the antioxidant activity by scavenging capacity of the assay by ABTS and DPPH. Was also developed a methodology for obtaining the compounds (S)-N-(alkyl-1-(3-aryl-1,2,4-oxadiazol-5-yl)-2-(phenylchalcogenide)acetamide derived from (S)-2-(2-(phenylchalcogenide)acetamido)alkanoic acids and arylamidoximes employing microwave irradiation. This synthesis was carried out in three conditions by varying the reaction time, temperature and solvent. The reactions employing microwave irradiation exhibit advantages against reactions using conventional method. These compounds were characterized by 1H NMR, 13C NMR and techniques high resolution mass spectrometry.
No presente trabalho, uma série de 2-alquil/arilcalcogeno-N-(4-aril-1,3-tiazol-2-il)acetamidas foi preparada via adição de calcogenetos de alquila ou arila. Essa metodologia permitiu a obtenção de derivados de 2-amino-1,3-tiazois em bons rendimentos. A proposta dessa síntese tem a finalidade de avaliar o potencial biológico a partir da atividade antioxidante por meio da capacidade sequestradora dos compostos sintetizados através de ensaios de ABTS e DPPH. Também foi desenvolvido uma metodologia para a obtenção dos compostos (S)-N-(1-(3-aril-1,2,4-oxadiazol-5-il)alquil)-2-(calcogenofenil)acetamidas derivados de ácidos (S)-2-(2-(calcogenofenil)acetamido)alcanoicos e arilamidoximas, empregando irradiação de micro-ondas. Para essa síntese foram desenvolvidas três condições reacionais variando o tempo reacional, temperatura e solvente. As reações conduzidas em micro-ondas apresentaram vantagens frente às reações em método convencional. Estes compostos foram caracterizados por técnicas de RMN 1H, RMN 13C e por espectrometria de massas de alta resolução.
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Fallan, Charlene. "Ytterbium-catalysed conjugate allylation of alkylidene malonates and enantioselective nickel-catalysed Michael additions of azaarylacetates and acetamides to nitroalkenes." Thesis, University of Edinburgh, 2012. http://hdl.handle.net/1842/7683.
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I. Catalytic Conjugate Allylation of Alkylidene Malonates Nucleophilic conjugate addition of allylsilanes and allylstannanes to alkylidene malonates under the action of ytterbium catalysis in the presence of hexafluoro-isopropanol has been developed. Enantioselective conjugate allylation of alkylidene malonates under ytterbium or scandium catalysis using chiral bis(oxazoline) ligands allows access to the conjugate addition products in an enantiomerically-enriched form. Furthermore, elaboration of the allylated substrates via decarboxylation and an oxidative cleavage was demonstrated. II. Catalytic Enantioselective Conjugate Addition of Azaarylacetates and Acetamides to Nitroalkenes An enantioselective nickel-catalysed Michael addition of azaarylacetates and acetamides to nitroalkenes has been developed. A range of azaaryl pronucleophiles were shown to react with a variety of nitroalkenes to generate highly functionalised Michael addition products with impressive diastereo- and enantiocontrol. A possible mechanism for this process is proposed and crystal structures of the addition products have also been attained, allowing determination of the absolute stereochemistry. Elaboration and further functionalisation of these products was also possible under a range of conditions.
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Gomes, Roberto da Silva. "Análise conformacional e das interações eletrônicas de algumas N-metóxi-N-metil-acetamidas-α-heterossubstituídas." Universidade de São Paulo, 2011. http://www.teses.usp.br/teses/disponiveis/46/46136/tde-31082011-144942/.
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A presente tese trata da síntese e a análise conformacional de algumas N-metóxi-N-metil-amidas α-heterossubstituídas (amidas de Weinreb) Z-C(O)-N(OMe)Me (Z= CH2F (1), CH2OMe (2), CH2OPh (3), CH2Cl (4), CH2Br (5), CH2SEt (6) e Me2CSEt (7). A análise da banda da carbonila no infravermelho apoiada por cálculos teóricos B3LYP/6311++G(3df, 3pd), juntamente com a análise de NBO indicou a existência de um equilíbrio conformacional cis/gauche, isto é, (c) e (g) para (1) e (3), (c1, c2) e (g1, g2) para (2), (c) e (g1, g2) para (4-6) e (g1, g2) para (7). Em fase gasosa a população do confôrmero gauche prevalece ligeiramente sobre a população do confôrmero cis para os compostos (1) e (3); a população de (c1 + c2) prevalece sobre a população de (g1 + g2) para o composto (2) e a soma das populações de (g1 + g2) é mais abundante que a população de (c) para os compostos (4), (5) e (6). Já para o composto (7) a população do confôrmero g1 prevalece sobre a do g2. Nos compostos (4), (5) e (6), em solução de n-hexano, a ocorrência da ressonância de Fermi na região da vibração de estiramento da carbonila (VCO), impede qualquer estimativa das populações relativas dos confôrmeros (c, g1 e g2). Já, no composto (7) constata-se, em n-hexano, somente a presença do confôrmero (g1). Os resultados dos espectros da banda do composto (7), que contém duas metilas ligadas ao carbono α exclui a possibilidade da ocorrência da ressonância de Fermi. Os cálculos SCI-PCM concordam com o efeito do solvente sobre a intensidade relativa dos componentes da banda da carbonila para os compostos (1-3). A análise de NBO mostrou que a interação orbitalar nN→π*CO é o principal fator que estabiliza o confôrmero gauche (g, g1,e g2) em maior extensão do que o confôrmero cis (c, c1 e c2) para os compostos de (1-6). As interações orbitalares nY→π*CO, σC-Y→π*CO, πCO→σ*C-Y e π*CO→σ*C-Y também contribuem para a estabilização do confôrmero gauche (g, g1, g2) em relação ao confôrmero cis (c, c1, c2), porém em menor extensão. A existência de uma piramidalização no átomo de nitrogênio das amidas de Weinreb é responsável pela ocorrência dos contatos curtos entre Yδ-(4)…Oδ-(9) e Yδ-(4)…Nδ-(7) nos confôrmeros gauche (g, g1, g2), que origina uma forte interação coulombica repulsiva, agindo fortemente em oposição à estabilização dos confôrmeros gauche (g, g1, g2) em relação aos confôrmeros cis (c, c1, c2). Portanto, um delicado equilíbrio entre as interações Coulômbicas e as interações orbitalares, pode ser responsável pela estabilização observada nos confôrmeros cis (c, c1, c2) em relação aos confôrmeros gauche (g, g1, g2), tanto em fase gasosa, quanto em solução. Contrariamente ao que seria esperado, a predominância do confôrmero cis (em solução de n-hexano e tetracloreto de carbono) para as N-metóxi-N-metil amidas α-heterossubstituídas (1-3), contendo em α-átomos da primeira fila (flúor e oxigênio) está em direção oposta à preferência do confôrmero gauche para as N-metóxi-N-metil amidas α-heterossubstituídas remanescentes (4-6) contendo em α átomos da segunda e terceira filas (cloro, enxofre, bromo), onde os confôrmeros g1 e g2 são preponderantes ou exclusivos no caso de (7).This thesis deals with the synthesis and conformational analysis of some α-heterosubstituted N-methoxy-N-methyl-amides (Weinreb amides) Z-C(O)-N(OMe)Me (Z= CH2F (1), CH2OMe (2), CH2OPh (3), CH2Cl (4), CH2Br (5), CH2SEt (6) and Me2CSEt (7). The analysis of the carbonyl band in the IR spectra supported by B3LYP/6 311++G(3df, 3pd calculations along with the NBO analysis indicated the existence of a cis-gauche conformational equilibrium i.e. (c) and (g) for (1) and (3), (c1, c2) and (g1, g2) for (2), (c) and (g1, g2) for (4-6) and (g1, g2) for (7). In the gas phase the g conformer population prevails slightly over the c one for (1) and (3); the (c1 + c2) population prevails over the (g1 + g2) for (2), and the (g1 + g2) conformer population is more abundant than the population (c) for (4), (5) and (6). In n-hexane solution the cis conformer is more abundant for (1-3). The occurrence of Fermi resonance in the VCO region, in n-hexane, precludes the estimative of relative populations of the (c, g1, g2) conformers for (4-6). The SCI-PCM calculations agree with the solvent effect on the VCO band component relative intensities for (1-3). NBO analysis showed that the nN→π*CO orbital interaction is the main factor which stabilizes the gauche (g, g1, g2) conformers for (1-6) into a larger extent relative to the cis (c, c1, c2) ones. The nY→π*CO, σC-Y→π*CO, πCO→σ*C-Y and π*CO→σ*C-Y orbital interactions still contribute, but into a minor extent for the stabilization of the gauche conformers relative to the cis ones. The existence of some pyramidalization at the nitrogen atom of the Weinreb amides (1-6) is responsible for the occurrence of Yδ-(4)…Oδ-(9) and Yδ-(4)…Nδ-(7) short contacts in the gauche (g, g1, g2) conformers, which originates strong repulsive Coulombic interactions, acting in opposition to the large orbital stabilization of the gauche conformer with respect to the cis one. The same effects are responsible for the larger stabilization of the (g1, g2) conformers of (7) which in turn precludes the existence of the c conformer. Therefore, a delicate balance of the Coulombic and orbital interactions seems to be responsible for the observed stabilization of the gauche (g, g1, g2) and cis (c, c1, c2) conformers, both in the gas phase and in the solution for (1-6) and (7). However, the cis conformer predominance, in non polar solvents, for the α-substituted N-methoxy-N-methyl acetamides (1-3), bearing in α first row (fluorine and oxygen) atoms, is in the opposite direction to the gauche conformer preference for the remaining α-substituted N-methoxy-N-methyl acetamides (4-6), bearing in α second and third rows (chlorine, sulfur, bromine) atoms. However the g1 and g2 conformers are the only ones present for (7).
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Alcantara, Edesio Fernandes da Costa. "Acetilacetona, diacetamida e N-(2-piridil)-acetamida imobilizadas na superficie de silica gel - preparação, caracterização, adsorção, termoquimica e espectroscopia de complexos suportados." [s.n.], 1993. http://repositorio.unicamp.br/jspui/handle/REPOSIP/250065.
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Orientador : Claudio AiroldiTese (doutorado) - Universidade Estadual de Campinas, Instituto de Quimica
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Santana, Rafael Germano [UNIFESP]. "Análise conformacional e das interações eletrônicas de algumas 2-acetamido-3-metil-3-nitrososulfanil-N-arilbutanamidas: S-nitrosotióis com potencial atividade biológica." Universidade Federal de São Paulo (UNIFESP), 2012. http://repositorio.unifesp.br/handle/11600/8899.
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Publico-13280.pdf: 1828173 bytes, checksum: df8fb9928c37e920c5f9a2281ba9c092 (MD5)O presente trabalho trata do estudo conformacional de S-nitrosotióis com potencial atividade biológica, 2–acetamido-3-metil-3-nitrosossulfanil-N-arilbutanamidas, e de seus tióis precursores, 2–acetamido-3-mercapto-3-metil-N-arilbutanamidas. As conformações de menor energia dos S-nitrosotióis e tióis em estudo são estabilizadas por ligações de hidrogênio intramoleculares que promovem uma maior estabilidade dos confôrmeros. A análise geométrica do grupo R-SNO mostra que esses compostos preferem a conformação trans. O cálculo das interações orbitalares pelo método NBO (Natural Bond Orbital) para as 2–acetamido-3-mercapto-3-metil-N-arilbutanamidas mostrou que as mesmas são estabilizadas pelas seguintes interações: no (N2) → (C3-O4) e no(N10) → (C11-O12). Os resultados de NBO para os S-nitrosotíois mostraram que a interação hiperconjugativa é bastante efetiva nas conformações estáveis desses compostos, enfraquecendo a ligação que resulta no aumento do comprimento da ligação S-N em S-Nitrosotióis. A forte delocalização , induz caráter parcial a ligação S-N. A fraca ligação S-N indica uma forte delocalização do par de elétrons do O(NO) devido a interação, que é responsável pelo alongamento da ligação S-N, aumentando e a potencial capacidade do óxido nítrico ser liberado.
We carried out a conformational study on the S-nitrosothiols (R-SNO), 2-acetamido-3-methyl-3-(nitrososulfanyl)-N-arylbutanamides and their thiol precursors 2-acetamido-3-mercapto-3-methyl-N-arylbutanamides. The lowest energy conformation for both compounds is stabilized by intramolecular hydrogen bonds. Trans conformation was determined as the predominant conformation after geometrical analysis of R-SNO. Orbital interactions for 2-acetamido-3-mercapto-3-methyl-N-arylbutanamides were calculated using Natural Bond Orbital (NBO) methodology. Calculations indicated that orbital interactions for these compounds are stabilized by the following interactions: no (N2) → (C3-O4) and no(N10) → (C11-O12). NBO results showed that the hyperconjugative interaction is very effective, weakening the σ bond and resulting in increasing length of the S-N bond in R-SNO. The strong delocalization induces partial character to the S-N bond. The bond S-N indicates a strong delocalization of the electron pair of O(NO) due to interaction. This interaction is responsible for the elongation of the S-N bond which increases the ability of the compound to release nitric oxide (NO). Based on the enhanced capacity to release NO by these compounds, our findings suggest that both compounds may display biological activity.
TEDE
BV UNIFESP: Teses e dissertações
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Liang, Hong. "A short synthetic route to derivatives of 2-acetamido-4-amino-2,4,6-trideoxy-D-galactose, a component of the cell surface of Streptococcus peneumoniae." Thesis, National Library of Canada = Bibliothèque nationale du Canada, 2000. http://www.collectionscanada.ca/obj/s4/f2/dsk1/tape3/PQDD_0012/MQ60681.pdf.
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Ben, Tiba Younes. "Synthèse d'analogues iodés du practolol." Université Joseph Fourier (Grenoble), 1997. http://www.theses.fr/1997GRE10269.
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Les etudes biologiques ont montre qu'un derive du practolol dans lequel le groupe acetamido en para a ete remplace par hncoch#2ch#2ch=chi (ami-9), possede les caracteristiques necessaires a un marqueur des recepteurs -adrenergiques. La synthese de l'enantiomere s (la seule forme active) et marque avec une haute activite specifique a constitue le premier objectif de ce travail. Pour verifier la purete enantiomere avec laquelle ami-9s a ete obtenu, nous avons mis au point une methode de determination de cette purete a l'aide d'un agent de derivation chiral, l'acide 2-fluoro-2-phenylacetique. Cette methode peut etre generalisee aux -bloquants du groupe b et etendue a la determination de la configuration des -aminoalcools. Le second objectif consistait a preparer de nouveaux analogues iodes du practolol en changeant les substituants soit sur l'azote de la fonction amine soit sur celui de la partie amide : - le groupe isopropyle par ch#2ch=chi et (ch#3)#2cch=chi, - le groupe nhcoch#3 par ich=chch#2ncoch#3 et hncooch#2ch=chi. Un dernier compose dans lequel la modification porte sur les deux azotes, en remplacant l'isopropyle par un groupe comportant la structure de la salicylamide et l'acetamido en para par hncoch#2ch#2ch=chi, a egalement ete synthetise.
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Rabuka, David. "Synthesis and NMR characterization of the six regioisomeric mono-O-phosphates of octyl 2-acetamido-2-deoxy-4- O-(ß-D-galactopyranosyl)-ß-D-glucopyranoside." Thesis, National Library of Canada = Bibliothèque nationale du Canada, 2000. http://www.collectionscanada.ca/obj/s4/f2/dsk1/tape3/PQDD_0012/MQ59868.pdf.
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Anderson, Kirstin P. C. "Development of an alternative synthesis of 2-acetamido-2-deoxy-L-altruronic acid: an unusual sugar found in the O-specific polysaccharide of Shigella sonnei." Master's thesis, University of Cape Town, 2017. http://hdl.handle.net/11427/24464.
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A new synthetic route has been explored for the preparation of derivatives of 2-acetamido-2-deoxy-L-altruronic acid (L-AltNAcA). This is a rare sugar found together with 2-acetamido-4-amino-2,4-dideoxy-D-fucose(D-FucNAc4N) in the repeating unit of Shigella sonnei. Derivatives are needed inter alia for chemical and spectroscopic calibration standards, and as building blocks for preparing oligomeric subunits of the O-polysaccharide antigen for possible incorporation into a synthetic glycoconjugate vaccine. Two synthetic routes were investigated. The first route successfully repeated a published four step sequence converting diacetone-D-glucose to 1,6-anhydro--L-idopyranose in a 38% yield overall, and a further selective benzylation at O-3. Attempts to discriminate between O-2, O-3 and O-4 using low temperature acylation or alkylation conditions were unsuccessful, but modest selectivity for the 4-benzoate was observed in a Bu₂SnO-mediated benzoylation, although this product could not be easily separated from other mono-benzoates. The second route started from N-acetyl-D-glucosamine which was successfully converted in the first step to 2-methyl-(1,2-dideoxyl-5,6-O-isopropylidene-α-D-glucofurano)-[2,1-d]-2-oxazoline. The oxazoline and dioxolane units could be selectively manipulated in a series of steps to afford 2-acetamido-2-deoxy-3-O-benzyl-6-O-t-butyldimethylsilyl-α-D-glucofuranosyl acetate in a 41% yield over four steps. This is a key synthetic intermediate in which the 5-OH is available for the required inversion step. During this study, an unusual minor side-product, 1,6-anhydro-2-acetamido-O-acetyl-2-deoxy-3-O-benzyl-α-D-glucofuranose, was isolated. While this was also a potentially useful intermediate, having only the 5-OH unprotected, it proved not possible to find conditions for optimizing this product. Inversion of configuration at C-5 in the 6-O-silylated glucofuranose was attempted via the 5-O-triflate and 5-O-mesylate: the triflate formed but was displaced in situ by the solvent pyridine to give an unusual 5-pyridinium derivative, while the mesylate was stable but unreactive towards subsequent SN2 inversion. These outcomes were attributed to the steric congestion imposed by the combination of the 3,4-cis-disubstitution of the furanose ring and the very bulky silyl substituent at O-6. While the goal of preparing L-AltNAcA was not achieved via these approaches, useful insights have been contributed towards the ongoing study.
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Bezerra, Fernando Antonio Frota. "Estudo fase I do cloridrato do (1R, 2R)-(+)-N-metil-N-[2 (1-pirrolidinil) ciclohexil] benzo [B] tiofeno-4-acetamida (RSD921) em voluntarios sadios do sexo masculino." [s.n.], 1999. http://repositorio.unicamp.br/jspui/handle/REPOSIP/309478.
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Orientador: Gilberto de NucciDissertação (mestrado) - Universidade Estadual de Campinas, Faculdade de Ciências Médicas
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Resumo: O presente trabalho,um ensaio clínico Fase I, aberto, com doses únicas crescentes. teve como propósitos avaliar, em voluntários humanos sadios, a tolerância, a segurança, possíveis efeitos farmacodinâmicos e o perfil farmacocinético do Cloridrato de (1R,2R) -(+)¬N-metil- N- [2-(1-pirrolidinill) ciclohexil] benzo [b] tiofeno-4-acetamida (RSD921). 18 voluntários sadios, masculinos, foram escolhidos após avaliação através de exame clínico, exames cardiológicos e exames de patologia clínica. O estudo consistiu de uma infusão intravenosa, por 15 minutos, de RSD921, administrado em doses crescentes por três ocasiões diferentes. A dose máxima administrada foi de 1110 (0,02 mg/kg) da dose de segurança (0,2 mg/kg) em animais de laboratório. Amostras de plasma e urina foram colhidas antes da infusão da droga e a intervalos frequentes até 24 horas após infusão. Nesse período os voluntários foram clinicamente observados e o seu eletrocardiograma continuamente monitorizado e registrado em um sistema Holter de eletrocardiografia. Exames clínicos e laboratoriais foram repetidos após cada infusão de RSD921. Um voluntário (VoI.II-UNN) apresentou sintomas alérgicos caracterizados por conjuntivite e rinite durante a segunda infusão (dose de 0,0004 mg/kg), posteriormente classificado como não relacionado a droga em teste, determinando porém, uma modificação do protocolo de modo que todos os voluntários restantes receberam em seu primeiro intemamento uma infusão de RSD921 na dose de 0,0004 mg/kg. Nenhum outro voluntário relatou sintomas ou sinais alérgicos durante ou após administração do RSD921. Um outro voluntário, (VoI. XIV-AFA), apresentou significante hematúria apenas após a segunda infusão de RSD921, tambem não atribuida ao RSD921. Nenhuma hematúria foi observada após a terceira infusão de RSD921. Nenhuma outra alteração clínica, laboratorial e eletrocardiográfica considerada de relevância foi detectada ou relatada durante ou após infusão da droga nos voluntários, permitindo concluir que o RSD921 foi seguro e bem tolerado até a dose de 0,02 mg/kg, quando administrado por infusão intravenosa durante 15 minutos. As concentrações plasmáticas de RSD921 foram quantificadas por cromatografia líquida de alta pressão acoplada a espectrometria de massa.Os gráficos semi-logarítmicos de concentrãção plasmática versus tempo permitiram a conclusão de que a distribuição da droga não obedeceu ao modelo teórico de um compartimento, sendo mais consistente com o modelo de dois compartimentos. As variáveis farmacocinéticas AUC, Cmax; tl/2; ke, V d; foram calculadas a partir das curvas de concentração plasmática versus tempo. CL, t1/2 klO para os compartimentos alfa e beta, VI e Vss foram calculados utilizando o modelo teórico de dois compartimentos. A linearidade farmacocinética foi aceita com base na correlação entre AUC, ke e tl/2 versus dose total administrada. 95% de intervalo de confiança para o coeficiente r de Pearson foram -0,47 a 0,005; -0,17 a 0,037 e 0,78 a 0,92 para; ke, tl/2 e AUC versus Dose Total Administrada, respectivamente, permitindo concluir que o RSD921 apresenta farmacocinética linear ou de 1 a ordem
Abstract: The aim of the study was to evaluate, on healthy human male volunteers, the tolerance, the safety, pharmacokinetic profile, and some pharmacodynamic effects of the compound (IR, 2R)-( +)-N-methyl-N- [2-(I-pyrrolidinylI)cyclohexyl]benzo[b ]tiophene-4¬acetamide monohydrochloride (RSD921) administered as a single dose. The study was an open, stepwise-ascending dose. Eighteen healthy male volunteers, as assessed by clinical and laboratory test evaluations, were emolIed onto the study. The study consisted in a fifteen-minute intravenous infusion RSD921, administered in three different occasions. The maximum dose reached was 1/10th of that considered safe (0.2 mg/kg) in laboratory animaIs. Plasma and urine samples for RSD921 determination were obtained pre-dose and up to 24 hours post-dosing. During the infusion period and until 24 hours post-dosing the volunteers were continuously monitored by fulI Holter electrocardiography. Clinical and laboratory test evaluations were repeated folIowing each infusion. One volunteer presented alIergic symptom characterised by conjunctivitis and rhinitis during the second infusion (I/500) of RSD921 that lasted two hours after the infusion. The same dose was repeated in a week later, and was not accompanied by any clinical sign or symptom of alIergy. A protocol modification was introduced and alI volunteers (but the last one) received first an infusion of 1/500 before proceeding to the next dose. No other volunteer reported alIergic symptoms or signs during or after RSD921 administration. One volunteer presented. haematuria after the second infusion of RSD921. The volunteer did report that had sexual intercourse one hour before colIecting the urine sample. The volunteer presented no haematuria after the third infusion RSD921. No other significant clinical or laboratory alteration was either reported or detected folIowing RSD921 infusion in the volunteers. In conclusion, RSD921 up to the dose of 0.02 mg/kg was safety and welI tolerated by alI volunteers when administered intravenously in a fifteen-minute infusion. RSD921 plasma concentrations were quantified by a validated method employing high-pressure liquid chromatography coupled to mass spectrometry (LC-MS-MS). As plasma concentration of RSD921. versus time (starting at maximum concentration attained) in a semi-Iogarithmic plot did not show a straight-line, it could b~ conclude that the data did not agree with one-compartment theory model. Goodness of fit did not show statistical difference between two- or three¬compartment model. The sum of squared residual was less for two- than for three¬compartment model and it has shown smalIer degree of freedom (one less variable for two¬compartment model), therefore it gave more consistence to the two-compartment theoretic model. From the plasma samples, the area under the curve (AUC), the maximum concentration attained (Cmax), the elimination half-life, the elimination constant (Ke) and the distribution volume (V d) were calculated with the observed values. Clearance (CL), alpha, beta and KlO half-lives (t1/2), volume of compartment 1 (VI) and volume of distribution at the steady state (Vss) were calculated assuming the two-compartment theoretic model. 95% CI for Pearson's r coefficient were -0.47 to 0.05, -0.17 to 0.37 and 0.78 to 0.92, for Ke, t1/2 and AUC versus Total Dose Administered, respectively. Pharmacokinetic linearity was accepted in the basis of correlation between AUC and Ke and t1/2 versus Total Dose Administered.
Mestrado
Mestre em Farmacologia
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Subtil, Fernanda Teixeira. "Identifica??o do alvo molecular das 2(quinolin-4-il?xi) acetamidas como candidatos a f?rmacos para o tratamento da tuberculose." Pontif?cia Universidade Cat?lica do Rio Grande do Sul, 2017. http://tede2.pucrs.br/tede2/handle/tede/7359.
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Coordena??o de Aperfei?oamento de Pessoal de N?vel Superior - CAPES
The high incidence of tuberculosis is a great concern worldwide. Different strategies are being developed by the World Health Organization to fight tuberculosis. Amongst the three pillars that are part of the End TB Strategy, we can highlight the intensive research and innovation pillar. In this extent, the development of new drugs for tuberculosis treatment is a field that is gaining importance. The 2(quinolin-4-yloxy) acetamides are molecules that showed promising bactericidal effects in Mycobacterium tuberculosis, which motivated us to continue studying to improve their mycobactericidal activity and also perform their chemical and biological characterization. In order to continue the 2(quinolin-4-yloxy) acetamides derivatives development, the target identification of these molecules is a keystone and is also the focus of this study. Initially, it was hypothesized that DNA gyrase was their molecular target due to the great chemical similarities between the 2(quinolin-4-yloxy) acetamides and the fluoroquinolones. Despite our results that the 2(quinolin-4-yloxy) acetamides have diminished effects in ofloxacin resistant clinical isolates, the results obtained with the gyrA point mutant and with DNA gyrase protein revealed that this enzyme is not the molecular target of these compounds. The new target identification strategy involved the selection of spontaneous mutants for our lead compound 12L, characterization of this mutant strain against other 2(quinolin-4-yloxy) acetamides derivates and whole genome sequencing. Whole genome sequencing data allowed the identification of a single mutation (T313A) in the QcrB protein, which is the B subunit of cytochrome bc1 complex. This mutation was confirmed by Sanger sequencing and molecular docking results confirmed the importance of this residue for proteindrug interaction. The cytochrome bc1 complex is involved in the electron transport of the bacilli?s respiratory chain, and therefore it appears to be an interesting target, especially to treat the latent form of the disease. We hope that this work contributes to the 2(quinolin-4-yloxy) acetamides development for tuberculosis treatment.
A alta incid?ncia da tuberculose, em ?mbito mundial, ? de grande preocupa??o. Para combater esta doen?a, diferentes estrat?gias v?m sendo desenvolvidas pela Organiza??o Mundial da Sa?de (OMS). Dentre os pilares que comp?em a End TB strategy, podemos destacar a pesquisa intensiva e a inova??o. Neste ?mbito, o desenvolvimento de novos f?rmacos para tuberculose vem ganhando destaque. As 2(quinolin-4-il?xi) acetamidas s?o mol?culas que demonstraram resultados bactericidas promissores frente ao Mycobacterium tuberculosis, o que nos motivou a realizar novos estudos para melhorar a atividade e realizar a caracteriza??o qu?mica e biol?gica destas mol?culas. A fim de continuar o desenvolvimento da s?rie quinol?nica, a identifica??o do seu alvo molecular foi o foco deste trabalho. Inicialmente, levantou-se a hip?tese de que a DNA girase seria o alvo molecular, uma vez que as 2(quinolin- 5-il?xi) acetamidas possuem grande similaridade estrutural com as fluoroquinolonas. Apesar das 2(quinolin-4-il?xi) acetamidas terem apresentado menor atividade frente a isolados cl?nicos resistentes a ofloxacino, os resultados de atividade obtidos frente a uma mutante pontual de gyrA e frente ? prote?na indicam que a DNA girase n?o ? o alvo destas mol?culas. A nova estrat?gia para identifica??o de alvo envolveu a sele??o de mutantes espont?neos para o composto l?der 12L, caracteriza??o desta cepa frente aos demais compostos da s?rie e sequencimento total do genoma. Este permitiu a identifica??o de uma ?nica muta??o (T313A) localizada na prote?na QcrB, que ? a subunidade B do complexo citocromo bc1. Esta muta??o foi confirmada por sequenciamento de Sanger e o docking molecular aferiu a import?ncia deste res?duo na intera??o prote?na-composto. O complexo citocromo bc1 est? envolvido no transporte de el?trons na cadeia respirat?ria do bacilo, e por isso ? um alvo molecular interessante, principalmente para combater a forma latente da doen?a. Esperamos que este trabalho contribua no processo de desenvolvimento das 2(quinolin-4-il?xi) acetamidas para o tratamento da tuberculose.
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Flanigan, David L. "Studies in rhodium catalyzed intramolecular C-H insertion of amino acid derived [alpha]-diazo-[alpha]-(substituted)acetamides and its application to the total synthesis of clasto-lactacystin [beta]-lactone." [Tampa, Fla.] : University of South Florida, 2004. http://purl.fcla.edu/fcla/etd/SFE0000418.
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Murphy, Deirdre M. "STUDIES OF THE METALLO BETA LACTAMASE CCrA FROM BACTERIODES FRAGILIS AND A DANSYLATED MONOCYCLIC BETA LACTAM (1-(5-DIMETHYLAMINO-1-NAPTHALENESULFONYL HYDRAZIDO)-3-ACETAMIDO-4-METHOXY-2-AZETIDINONE." University of Cincinnati / OhioLINK, 2001. http://rave.ohiolink.edu/etdc/view?acc_num=ucin990561318.
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Flanigan, David L. Jr. "Studies in Rhodium Catalyzed Intramolecular C-H Insertion of Amino Acid Derived α-Diazo-α-(substituted)acetamides and its Application to the Total Synthesis of clasto-Lactacystin β-Lactone." Scholar Commons, 2004. https://scholarcommons.usf.edu/etd/1037.
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Lactacystin is a microbial metabolite isolated by Omura that exhibits neurotrophic activity in neuroblastoma cell lines. Lactacystin and especially its β-lactone analog are the first examples of non-polypeptide small molecules capable of specifically inhibiting the 20S proteasome. Various asymmetric total syntheses of lactacystin and its analogs have been reported. The total synthesis of clasto -lactacystin β-lactone is achieved using L-serine methyl ester as the starting material and the sole source of stereochemical induction. The success of this synthesis hinges on two featured transformations. The first key step involves formation of the γ -lactam core via rhodium (II) catalyzed intramolecular C-H insertion of the α-diazo-α-(phenylsulfonyl)acetamide intermediate. The methodology for this transformation has been developed and applied to the synthesis of highly functionalized stereogenic γ-lactams from natural α-amino acids. Three control elements that govern γ-lactam formation are described. This step is highlighted by the xvi simultaneous creation of two stereogenic centers of the γ-lactam core. The second key step involves the late stage aldol coupling for quaternary carbon formation and installation of the hydroxyisobutyl group. In all previously reported syntheses, this is the very first aspect which is addressed. The stereochemical outcome of this step is directed by the chiral environment of the enolate itself. Various attempts to achieve selectivity are explored and reported. Completion of the synthesis of clasto-lactacystin β-lactone requires 17 steps with an overall yield of 10%. Some general attempts for optimizing the synthetic scheme are discussed as well as the future direction of this research.
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Gavel, Marine. "Nouveaux développements chimiques pour la conception d'inhibiteurs de glycosyltransférases Carbene-mediated quaternarization of the anomeric position of carbohydrates: synthesis of allylic ketopyranosides, access to the missing α-gluco and β-manno stereoisomers, and preparation of quaternary 2-deoxy 2-acetamido sugars Regio- and chemoselective deprotection of primary acetates by zirconium hydrides." Thesis, Normandie, 2019. http://www.theses.fr/2019NORMIR09.
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Ces travaux de thèse ont été consacrés au développement de voies de synthèses permettant l'obtention de structures cétopyranosidiques modulables en vue du développement d'outils chimiques dédiés à la glycobiologie. Nous avons tout d'abord travaillé au déploiement de séquences réactionnelles ouvrant l'accès à des glycophosphomimétiques possédant une unité triméthylène phosphonate. Par ailleurs, nous avons mis au point une nouvelle méthode de déprotection régiosélective de la position primaire de sucres peracétylés utilisant un mélange bimétallique de zirconium et d'aluminium permettant de faciliter l'accès à des (oligo)saccharides ayant des liens glycosidiques α-1,6. Enfin, en combinant ces développements chimiques, nous avons souhaité préparer des inhibiteurs potentiels de glycosyltransférases bi-substrats possédant à la fois un mime du groupe partant du donneur de glycosyle et de l'accepteur connectés à la position anomère quaternaire des cétopyranosidesThe goal of this project is to challenge the hypothesis that a non-natural sugar with a quaternary anomeric position might be the central core of a powerful and selective inhibitor of glycosyltransferase. Our design is relying on a key quaternary anomeric centre that provide the unique opportunity to incorporate in a single innovative structure the acceptor, the donor and the leaving group released during the formation of the glycosidic linkage. The functionnalization of the ketopyranosides that will be at the centre of this new class of potent glycosyltransferases inhibitors rely on original synthetic methods allowing introduction of a trimethylene phosphonate and regioselective deprotection of primary position of acetylated sugars for building alpha-1,6 glycosidic linkages
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BICHARA, MARC. "Mutagenese induite par une amine aromatique cancerogene et sa reparation chez e. Coli." Université Louis Pasteur (Strasbourg) (1971-2008), 1986. http://www.theses.fr/1986STR13157.
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Chen, Shau-Chang, and 陳紹昌. "Syntheses and Characterizations of Acetamide Fuctionalized Imidazolium Metals Complexes." Thesis, 2005. http://ndltd.ncl.edu.tw/handle/74116675462032575843.
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Chuan, Yang Pi, and 楊碧娟. "Metallomesogens Based on Acetamide and Carboxylate Functionalized Imidazolium Salts." Thesis, 2002. http://ndltd.ncl.edu.tw/handle/10850325567114937252.
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碩士輔仁大學
化學系
90
Abstract Amide functionalized of N-heterocyclic carbene complexes of silver(I) and gold(I) were prepared. All the complexes prepared are thermotropic liquid crystals. These compounds also exhibit gellating properties in DMSO. Porous donut shaped solids composed of fibers of 260nm thickness were obtained from MeOH solvent. Interesting thermochromism phenomenon occurs in the phase transition. A helical structure were proposed. Liquid crystalline zinc(II) and copper(II) complexes of carboxylates containing imidazolium cations were prepared. Liquid crystalline behaviors of these compounds are different from those simple carboxylate compounds, because of the zwitter ionic properties of the ligands we used. The Cu(II) series trends to form lamellar mesophase instead of discotic mesophase observed in the carboxylate compouns.
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Wang, Kai Dei, and 王凱迪. "Study of Corrosion Resistance of AZ91D Alloy by Dimethyl Acetamide." Thesis, 2011. http://ndltd.ncl.edu.tw/handle/01912277312146989031.
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碩士高苑科技大學
化工與生化工程研究所
99
Abstract Anodic oxide film on AZ91D ally was prepared by micro-ace oxidation process using pulse-reverse plating. The additive , Dimethyl acetamide ,in the plating solution is a key factor to improve the characteristic of anodic oxide film. When Dimethy acetamide concentration was adjusted at 0.12M,the anodic oxide film was formed in the plating solution with long passive potential of 12V and low corrosion current desity of 0.0158mA/cm2. Moreover , the hardness , thickness , and dense structure were also improved by the additive ,Dimeyhyl acetamide. Finally, the optimum operating condition, pulse-plating potential of 500V , reveres-plating potential of 50V , pulse-plating period of 50ms,reveres-plating of 50ms and 6000 duty cycles , could form the anodic oxide film with thickness of 113µm and 1763 HV.
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Chang, Meng-Ying, and 張孟縈. "Metallomesogens Based on Acetamide Functionalized Imidazolium Salts and Triazolium compounds." Thesis, 2006. http://ndltd.ncl.edu.tw/handle/83709818774475401025.
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李依婷. "Ionic Liquid Crystals of Acetamide and Acetic Acid Functionalized Imidazolium Salts." Thesis, 2003. http://ndltd.ncl.edu.tw/handle/08653759293450697007.
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碩士輔仁大學
化學系
91
Abstract： The aim of this work is to synthesize and investigate the liquid crystalline properties of unsymmetrical imidazolium salts containing amide (-CH2CONH2) and acid (-CH2CO2H) functionalized cations with anions of Br- , PF6-, and BF4-. Both liquid crystalline behavior of {[Cn-Im-CH2CONH2][Y]} and {[Cn-Im-CH2CO2H][Y]}, where n=10, 12, 14 ,16 , 18; Y=Br-, PF6-, BF4-, were studied by polarized optical microscopy, differential scanning calorimetry, and powder X-ray diffraction. Single crystal structure of [C12-Im-CH2CONH2][PF6] shows that this one self-organizes to form a frame work of hydrogen bonded ribbon polymer. The presence of extend hydrogen bonding interactions in these imidazolium salts allows them to have a wide temperature range of mesophase. Anions have a profound effect on the phase transition temperature, suggesting that both ionic and hydrogen bonding interactions play dominate roles in the mesomorphic behavior of these liquid crystalline compounds. Metal containing salts {[Cn-Im-CH2CONH2]2Pd2Br6}, where n=10, 12, were prepared.
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Yan-JhuChen and 陳彥竹. "Synthesis of Highly Substituted 2-Quinolinones via Intramolecular Cyclization of Acetamide Derivatives." Thesis, 2016. http://ndltd.ncl.edu.tw/handle/44316335157697510707.
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碩士國立成功大學
化學系
104
Three effective methods for the synthesis of 2-quinolinones were reported. We use α-substituted N-[2-(phenylethynyl)phenyl]acetamides as substrates, undergoes a 6-exo-dig cyclization and consequently produce 3,4-disubstituted 2-quinolinones. Surprisingly, heterocyclic substrates could also be used to generate the corresponding 2-quinolinones. To our delight, a variety of functional groups, including benzoyl, methoxycarbonyl and cyano groups, were used in these reaction conditions.
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Jhang, Heng-Cyuan, and 張恒銓. "The Study of Electrodeposited Molybdenum From Low Temperature Molten of Urea-Acetamide-MoCl5." Thesis, 2014. http://ndltd.ncl.edu.tw/handle/knz43h.
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Hsueh, Hsin-Hsueh, and 薛新學. "Synthesis and Characterization of Mercury with Acetamide Functionalized Imidazolium salts, Zwitterions and Metal Complexes." Thesis, 2007. http://ndltd.ncl.edu.tw/handle/q3nc36.
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蔣宇東. "Synthesis of 1-Benzyl Indole-3-acetamide and Related Compounds as Cell Differentiation Agent." Thesis, 2001. http://ndltd.ncl.edu.tw/handle/29576749079506140674.
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碩士中國醫藥學院
藥物化學研究所
89
As part of our continuing search for novel potentiators of the activity of retinoic acid in inducing differentiation of HL-60 cells, I have synthesized several analogs of the lead compound, indole-3-acetic acid. After testing the target compounds on HL-60 cells for differentiation and proliferation capability, a preliminary SAR was established.Most of the target compounds were found to be effective to potentiate the iuduction of different by retinoic acid.Among them, compound 1-benzylindole-3- acetamide (4), N-methyl-1-benzylindole-3-acetamide (5), N-ethyl-1- benzylindole-3-acetamide (6), N-n-propyl-1-benzylindole-3-acetamide (7),and N-methyl-1-benzylindole-3- carboxamide (13)showed most potent synesgistic activity and were selected for further evaluation.
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Cheng-HaoYang and 楊証皓. "Synthesis of Indol-2-ones from Acetamide Derivatives via Copper Ion Oxidative Free Radical Reaction." Thesis, 2016. http://ndltd.ncl.edu.tw/handle/55693761063028217269.
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碩士國立成功大學
化學系
104
According to the recent literatures, most of the methods use the radical initiator or metal to generate radical group. Afterward the radical group can undergo the addition reaction with unsaturated bond of the reactant, then the reactant do the cyclization to synthesis indol-2-one further. In this thesis, we synthesis the compounds which have a bromide group as reactants. We use the copper(II) acetylacetonate as an oxidant, and phenanthroline as a ligand to react with our reactant. The reactant may generate stably radical, and then that do cyclization reaction directly. The results show that we can use this method to synthesize a variety of indol-2-one derivatives, and this method is applicable to a variety of functional groups.