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VICENTE, Dmistocles de Andrade. "Reações de alilação e crotilação de diferentes aldeídos por trifluoroboratos orgânicos catalisada por aril-amidoximas." Universidade Federal Rural de Pernambuco, 2015. http://www.tede2.ufrpe.br:8080/tede2/handle/tede2/7049.
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First they were synthesized eight different aryl-amidoximes with moderate to excellent yields (35-91%). In parallel, the potassium allyltrifluoroborate and cis-crotyltrifluoroborate were synthesized also in good yields (78-75%). Properly synthesized and characterized the aryl-amidoximes and organic trifluoroborates, broke for studies of reaction conditions for the allylation of aldehydes. First, a study was made of the amount of benzamidoxime after a study of the best solvents proportion of water:dichloromethane. Established the lowest amount of the amidoxime and the best solvent system, broke to study the allylation reaction using different catalyst aryl-amidoximes. It was found that the p-bromobenzamidoxime showed the best result and the same was used in the continuation of studies. Established two reaction parameters (the aryl-amidoxime better and solvent system), left to the allylation reaction seventeen different aldehydes in which were found satisfactory results for the new method employed obtaining as a final product the homoallylic alcohols with moderate income excellent (40-93%). It was also carried out a study of chemoselectivity of the method, which has been verified the effectiveness of the method for obtaining the products of interest with good to excellent yields (75-93%). After these studies went up to the use of potassium cis-crotyltrifluoroborate under the same reaction conditions established in previous studies and also found themselves the effectiveness of the method for obtaining the products of interest with proceeds considered good to excellent (84-95% ).
Primeiramente foram sintetizadas oito diferentes aril-amidoximas com rendimentos de moderados a excelentes (35-91%). Em paralelo, foram sintetizados o aliltrifluoroborato e cis-crotiltrifluoroborato de potássio também com bons rendimentos (78-75%). Devidamente sintetizados e caracterizados as aril-amidoximas e os trifluoroboratos orgânicos, partiu-se para os estudos das condições reacionais para a alilação de aldeídos. Primeiramente, foi feito um estudo da quantidade de benzamidoxima, depois um estudo da melhor proporção de solventes água:diclorometano. Estabelecido a menor quantidade da amidoxima e o melhor sistema de solventes, partiu-se para o estudo da reação de alilação utilizando como catalisador diferentes aril-amidoximas. Constatou-se que a p-bromobenzamidoxima apresentou o melhor resultado e a mesma foi usada na continuidade dos estudos. Estabelecidos dois parâmetros reacionais (a melhor aril-amidoxima e sistema de solventes), partiu-se para a reação de alilação de dezessete diferentes aldeídos na qual foram encontrados resultados satisfatórios para o novo método empregado obtendo como produto final os alcoóis homoalílicos com rendimentos de moderados a excelente (40-93%). Foi realizado também um estudo de quimiosseletividade do método, no qual foi verificada a eficácia do método para a obtenção dos produtos de interesse com rendimentos de bons a excelente (75-93%). Após esses estudos partiu-se para o emprego do cis-crotiltrifluoroborato nas mesmas condições reacionais já estabelecidas nos estudos anteriores e verificou-se também a eficácia do método para obtenção dos produtos de interesse com rendimentos que considerados de bons a excelentes (84-95%).
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Tabélé, Clémence. "Réactions médiées par l'acétate de manganèse (III) et pharmacochimie antiparasitaire." Thesis, Aix-Marseille, 2016. http://www.theses.fr/2016AIXM5503.
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La leishmaniose est une maladie infectieuse due à Leishmania, responsable de plus de 50 000 décès par an en ce qui concerne la forme viscérale (LV). La plupart des médicaments antileishmaniens se révèlent inefficaces (apparition de résistances avec la molécule de référence : la pentamidine) ou trop onéreux pour les patients (incidence principale en Inde). Il existe donc un réel besoin de nouveaux médicaments ne manifestant aucune résistance parasitaire, moins chers et administrables par voie orale. Dans cet objectif, plusieurs séries de monoamidoximes (de structure similaire à celle de la pentadimine) ont été synthétisées, en utilisant des réactions radicalaires médiées par l'acétate de manganèse (III), et sous irradiation micro-ondes. Des réactions pallado-catalysées ont permis de diversifier les structures obtenues : couplages de Suzuki-Miyaura et couplages originaux avec des dérivés de structure allyl alcool. Plusieurs amidoximes ont ainsi montré une bonne activité in vitro sur les formes promastigote et amastigote de Leishmania et une faible toxicité sur des lignées de macrophages, leur indice de sélectivité étant meilleur que celui de la pentamidine, utilisée comme référenceLeishmaniasis is an infectious disease due to Leishmania : there are more than 50,000 deaths a year due to visceral form (VL). Most of antileishmanial drugs are either inefficient (too many resistances with the main drug : pentamidin) or too expensive for people (most of patients live in India). Thus, there is a real need for new drugs, without parasitical resistances, less expensive and orally administered. In this aim, several series of monoamidoxime, derivatives (pentamidine structure-like) have been synthesized using a free radical mechanism mediated by manganese (III) acetate under microwave irradiation. Palladium-catalyzed coupling reaction were also carried out for extensions of potential drugs : Suzuki-Miyaura reactions and original cross-coupling reactions involving allyl alcohol derivatives. Several amidoximes showed valuable in vitro activities toward Leishmania promastigote and amastigote forms,and low toxicity on macrophages, exhibiting a better selectivity index than pentamidine used as a drug compound reference
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Degardin, Mélissa. "Synthèse et activités antipaludiques de bis-alkylamidines N-monosubstituées, bis-alkylguanidines et de leurs bioprécurseurs de type amidoxime et O-dérivés." Montpellier 2, 2009. http://www.theses.fr/2009MON20165.
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Des stratégies prodrogues amidoxime et oxadiazolone ont été appliquées à de nouvelles drogues bis-alkylamidines N-monosubstituées que nous avons synthétisées selon une nouvelle stratégie divergente basée sur l'utilisation de la bis-alkyloxadiazolone N-substituée comme intermédiaire de synthèse. Des dérivés N-alkylsulfonyles de bis-alkylamidoximes ont été développés dans le but d'obtenir des structures stables in vitro tout en conservant de fortes activités orales. Enfin, de nouvelles drogues bis-alkylguanidines ont été synthétisées ainsi que leurs bioprécurseurs N-hydroxyguanidines, aminooxadiazolones et iminooxadiazolidinones. Les activités antipaludiques in vitro et in vivo des composés obtenus ont été évaluéesAmidoxime and oxadiazolone prodrug strategies have been applied to new N-monosubstituted bis-alkylamidine drugs which were synthesised by a new divergent strategy based on the use of the N-substitued bis-alkyloxadiazolone as an intermediate. Bis-alkylamidoxime N-alkylsulfonyles derivatives have been developed to obtain in vitro stable structures preserving potent oral activities. Finally, new bis-alkylguanidine drugs were synthesised as well as their bioprecursors N-hydroxyguanidines, aminooxadiazolones and iminooxadiazolidinones. In vitro and in vivo antiplasmodial activities of the obtained compounds were evaluated
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Sahyoun, Tanya. "Synthèse de double donneurs de monoxyde d’azote, évaluation de leur cytotoxicté et de leur activité pharmacologique." Electronic Thesis or Diss., Université de Lorraine, 2019. http://www.theses.fr/2019LORR0140.
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Ce travail décrit la synthèse de différentes familles de composés donneurs de monoxyde d’azote (NO) à base d’amidoximes ainsi que l’évaluation biologique de leur capacité à libérer NO. Dans un premier temps, la synthèse de double donneurs hybrides de NO portant conjointement une fonction amidoxime et une fonction S-nitrosothiol a été envisagée. Lors de ces essais, une molécule possédant deux fonctions amidoximes liées par un pont disulfure a été élaborée, avec pour objectif ultérieur sa réduction en thiol libre suivi d’une nitrosation par les enzymes des cellules. La suite des travaux a été consacrée à l’élaboration de différents types de donneurs de NO constitués uniquement d’amidoximes. Plusieurs mono-, bis- et poly-amidoximes ont été synthétisées et caractérisées. Toutes les amidoximes solubles dans le milieu physiologique ont été testées et se sont avérées cytocompatibles vis-à-vis de cellules musculaires lisses humaines. Les capacités de libération de NO et les cinétiques de ces libérations ont été évaluées. Finalement, les études biologiques visant à doser NO libéré ont montré que deux mono-amidoximes aromatiques permettaient de délivrer des quantités élevées de NO à la fois sur des microsomes de foie de rats et sur des cellules lisses humaines. Enfin, la bis-amidoxime aromatique/aliphatique présente une aptitude similaire à la libération de NO sur les cellules que les mono-amidoximes aromatiques mais à une concentration réduite de moitié, ce qui montre que cette molécule est la plus performante de tous les composés donneurs de NO testés dans le cadre de cette étudeThis work describes the synthesis of different families of nitritc oxide (NO) donor compounds based on amidoximes as well as the biological evaluation of their NO release ability. Firstly, the synthesis of hybrid NO double donors possessing jointly an amidoxime function and an S-nitrosothiol function has been considered. During these trials, a molecule having two amidoxime functions linked by a disulfide bond was developed, with a view to its subsequent reduction into free thiol followed by a nitrosation by the cells enzymes. The following part of this work has been devoted to the development of different types of NO donors consisting solely of amidoximes. Various mono-, bis- and poly-amidoximes have been synthesized and characterized. All the amidoximes that are soluble in the physiological medium have been tested and were shown to be cytocompatible with human smooth muscle cells. The NO release capabilities and the kinetics of these releases were evaluated. Finally, the biological studies aimed to evaluate the release of NO showed that two aromatic mono-amidoximes allowed providing high quantities of NO on both rat liver microsomes and on human smooth cells. Lastly, the aromatic/aliphatic bis-amidoxime presents a similar ability to release NO on cells as the aromatic mono-amidoximes but at a twice lower concentration, which shows that this molecule is the most powerful among all NO donor compounds tested during this study
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Kotthaus, Joscha [Verfasser]. "Metabolismus und Bioverfügbarkeit von Serinprotease-Inhibitoren und ihren Amidoxim-Prodrugs / Joscha Kotthaus." Kiel : Universitätsbibliothek Kiel, 2008. http://d-nb.info/1019622903/34.
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Froriep, Danilo [Verfasser]. "Reduktion N-oxygenierter Verbindungen durch die mitochondriale Amidoxim Reduzierende Komponente (mARC) / Danilo Froriep." Kiel : Universitätsbibliothek Kiel, 2013. http://d-nb.info/1031190384/34.
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Berger, Olivier. "Synthesis of antimalarial agents with new mechanisms of action." Thesis, Montpellier 2, 2010. http://www.theses.fr/2010MON20034.
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L'objectif de mon travail de thèse a été la synthèse de nouveaux agents antipaludiques afin de développer une nouvelle chimiothérapie pour lutter contre l'émergence de résistance multi-drogues de Plasmodium falciparum. Notre choix s'est porté sur le développement de trois nouvelles séries de composés: les quinolones qui inhibent le processus de respiration des mitochondries, les benzamidines qui inhibent la formation de l'hémozoïne et les alkylamidines qui bloquent le métabolisme phospholipidique. Dans le groupe du professeur O'Neill à Liverpool, la première partie de mon travail a été concentrée sur la synthèse de dérivés de 4-quinolone en faisant varier la chaîne latérale (chapitre II). La seconde partie de mon travail a été la synthèse de dérivés dibenzamidines en variant le linker hétérocyclique (chapitre III). Pour ce travail, le linker a été modifié: la chaîne alkoxy de la pentamidine a été remplacée par l'hétérocycle correspondant pour fournir les différentes séries de composés (thiazole, triazole, furane ou aziridine). Trois différents paramètres ont été étudiés pour ces dérivés: la position de la fonction amidine sur le cycle aromatique, l'angle entre les deux benzamidines et la position de l'hétérocycle au sein de la molécule. Pour tous ces composés, les activités antipaludiques in vivo ont été déterminées. Dans le groupe du professeur Durand à Montpellier, la première partie de mon travail a été la synthèse de dérivés alkylamidines en faisant varier le linker et en introduisant un noyau aromatique dans la tête polaire des reversed amidines. Le but était d'étudier l'influence du noyau aromatique sur l'activité antipaludique des drogues ainsi que le développement de leurs prodrogues (chapitre IV). Pour tous ces composés, les activités antipaludiques in vitro et in vivo ont été mesurées. La seconde partie de mon travail a été la réalisation des essais de stabilité et de bioconversion des différentes prodrogues dissymétriques (chapitre V). Les différentes conditions utilisées ont été optimisées sur la pentamidoximeThe objective of my PhD work was the synthesis of new antimalarial agents in order to develop a new chemotherapy to fight the emerging multi-drug resistant strains of Plasmodium falciparum malaria. Our choice has been the development of three new series of drugs: quinolones which inhibit the mitochondrial respiration process, benzamidines which inhibit hemozoin formation and alkylamidines which block phospholipid metabolism. Within the O'Neill group (Liverpool), the first part of my work has been focussed on the synthesis of 4-quinolone derivatives, varying the side chain (chapter II). The second part of my work has been the synthesis of dibenzamidine derivatives, varying the heterocyclic linker (chapter III). Within this work, the linker was modified in the following ways: alkoxy chain of pentamidine was replaced by the corresponding heterocycle to give four different series of compounds (thiazole, triazole, furane or aziridine). Three different parameters were studied for these derivatives: position of the amidine function on the aromatic ring, the angle between the two benzamidines and the position of the heterocyclic ring in the molecule. For these drugs, in vitro antimalarial activities have been measured. Within the Durand group (Montpellier), the first part of my work has been focussed on the synthesis of derivatives varying the linker of the bis-C-alkylamidines and introducing an aromatic ring in the polar head of the reversed amidines. The aim was to study the influence of the aromatic ring on the antimalarial activity of the drugs as well as the development of their prodrugs (chapter IV). For all these drugs and prodrugs, in vitro and in vivo antimalarial activities have been measured. The second part of my work has been based on the stability and bioconversion studies of different asymmetrical prodrugs (chapter V). The different conditions used for these studies have been optimised on the pentamidoxime
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Jakobs, Heyka Hellena [Verfasser]. "Studien zur Verknüpfung der mitochondrialen Amidoxim reduzierenden Komponente (mARC) mit dem Energiestoffwechsel / Heyka Hellena Jakobs." Kiel : Universitätsbibliothek Kiel, 2014. http://d-nb.info/1058586548/34.
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Ouattara, Mahama. "Chimiothérapie du paludisme : stratégie prodrogue pour des amidines actives par voie orale." Montpellier 1, 2003. http://www.theses.fr/2003MON13525.
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L'extension croissante de la chimiorésistance de Plasmodium vis à vis des antipaludiques actuels, nécessite une nouvelle approche chimiothérapeutique du paludisme. Dans ce cadre, notre étude est consacrée à l'amélioration de l'efficacité orale de nouvelles drogues amidiniques actives in vitro et in vivo sur Plasmodium. Nous avons préparé suivant une stratégie prodrogue, des carbamates d'amidines, des phosphonamidates d'amidines et des amidoximes. Par ailleurs, la synthèse de dérivés O-substitués d'amidoximes ainsi que des hétérocycles de type oxadiazolone et oxadiazole a été réalisée. Ces prodrogues potentielles d'amidine ont ensuite été évaluées sur un modèle murin de Plasmodium (P. Vincke/). Leur tolérance chez les souris a été déterminée. Ce travail a débouché sur des prodrogues de type amidoxime et analogues, a activité antiplasmodiale et efficaces par voie oraleThe increasing extension of the chemoresistance of Plasmodium to the current antimalarial drugs, requires a new chemotherapeutic approach of malaria. Within this framework of the research, our study is devoted to the improvement of the in vitro and in vivo oral effectiveness of new active amidinic drugs on Plasmodium. "We prepared according ta a prodrug's strategy, amidine carbamates, amidine phosphonamidates and amidoximes. We carried out the synthesis of O-substituted derivatives of amidoximes as weil as oxadiazolone and oxadiazole heterocycles. These potential prodrugs of amidine were also evaluated on a murine model of Plasmodium (P. Vinckel). Their tolerance in the mice was assessed. This approach led to amidoxime and analogs prodrugs with antiplasmodial activity and oral administration efficiency
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Krompholz, Nina [Verfasser]. "Reduktion von aliphatischen Amidoximen und N-hydroxylierten Basenanaloga durch neue molybdänhaltige Enzymsysteme / Nina Krompholz." Kiel : Universitätsbibliothek Kiel, 2013. http://d-nb.info/1031190414/34.
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BARROS, Carlos Jonnatan Pimentel. "Síntese e caracterização de 1,2,4-oxadiazóis e O-glicosídeos 2,3-insaturados inéditos." Universidade Federal Rural de Pernambuco, 2012. http://www.tede2.ufrpe.br:8080/tede2/handle/tede2/6317.
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In this work, we drescribed the synthesis and characterization of novel 1,2,4-oxadiazoles and 2,3-unsaturated glycosides, containing heterocyclic ring or terpene units as aglycone. The synthesis of alkyl and arylamidoximes was carried out using two methods: the first was using household microwave irradiation and the second in ultrasound-bath. The alkyl and arylamidoximes 18a-l were obtained with good yields and reduced time for the first two methods compared with the methods found in the literature. The new 1,2,4-oxadiazoles and bis-1,2,4-oxadiazoles were obtained by two methods: at reflux and by microwave irradiation. The 3-aryl-5-pentyl-1,2,4-oxadiazoles (46a-f) were obtained from methyl hexanoate. The bis-1,2,4-oxadiazoles 3,3’-aryl-5,5’-bis-1,2,4-oxadiazolyl propan-2-one (47a-h), 1,2-dihydroxy-1,2-bis [3-aryl-1,2,4-oxadiazol-5-yl]-ethane (48a-h) and 1,2-bis-(3-aryl-1,2,4-oxadiazol-5-yl)ethanol (49a-h) were obtained from the following esters, respectively: diethyl 3-oxoglutarate, dimethyl malate and diethyl tartarate. The novel 2,3-unsaturated O-glycosides were obtained from the Ferrier rearrangement of tri-O-acetyl-D-glucal with alcohols: 2-(3-thienyl)ethanol, citronellol and geraniol. The glycosides were subjected to reactions of basic hydrolysis and allylic oxidation. The structures of the compounds obtained were elucidated by conventional spectroscopic techniques: Infrared and Magnetic Nuclear Resonance 1H and 13C.
Neste trabalho, foi descrito a síntese e caracterização de inéditos 1,2,4-oxadiazóis e O-glicosídeos 2,3-insaturados, contendo anel heterocíclico ou unidades terpênicas como aglicona. A síntese de alquil e arilamidoximas foi realizada através de duas metodologias: a primeira consistiu na utilização de irradiação de microondas doméstico, a segunda em banho de ultrassom. As alquil e arilamidoximas 18a-l foram obtidas com bons rendimentos (40-92%) em tempos reduzidos quando comparado os dois primeiros métodos com os métodos encontrados na literatura. Os novos 1,2,4-oxadiazóis e bis-1,2,4-oxadiazóis foram obtidos através de duas metodologias: em refluxo e por irradiação de microondas. Os 3-aril-5-pentil-1,2,4-oxadiazóis (46a-f) foram obtidos a partir do hexanoato de metila e os bis-1,2,4-oxadiazóis 3,3’-aril-5,5’-bis-1,2,4-oxadiazolil propan-2-ona (47a-h), 1,2-diidroxi-1,2-bis[3-aril-1,2,4-oxadiazol-5-il]-etano (48a-h) e 1,2-bis-(3-aril-1,2,4-oxadiazol-5-il)-etanol (49a-h) foram obtidos a partir dos seguintes ésteres, respectivamente: 3-oxoglutarato de dietila, tartarato de dietila e malato de dimetila. Os O-glicosídeos 2,3-insaturados inéditos foram obtidos a partir do Rearranjo de Ferrier do tri-O-acetil-D-glucal com os álcoois: 2-(3-tienil)etanol, geraniol e citronelol . Os glicosídeos obtidos foram submetidos à reação de hidrólise básica e de oxidação alílica. As estruturas compostos obtidos foram elucidadas através de técnicas espectroscópicas convencionais: Infravermelho e Ressonância Magnética Nuclear de 1H e 13C.
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Weber, Philippe. "Synthèse et évaluation de nouveaux inhibiteurs de la fructose-1,6-diphosphate aldolase de classe II à zinc." Paris 11, 2003. http://www.theses.fr/2003PA112214.
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Le présent travail de recherche concerne la synthèse de nouveaux inhibiteurs d'une enzyme encore mal connue, la fructose 1,6-diphosphate (FdP) aldolase de classe II, très intéressante en tant que cible thérapeutique. Les deux classes de FdP aldolases se différencient par leur mode de fonctionnement très diffèrent et par les organismes dans lesquels ils se trouvent. Les aldolases de classe I sont présentes partout alors que les aldolases de classe II se trouvent uniquement dans les bactéries et les levures dont de nombreuses espèces pathogènes. En 1973, le phospho-glycolo-hydroxamate (PGH) s'est montré un très bon inhibiteur de cette enzyme in vitro. C'est le seul bon inhibiteur connu. Il y a donc de bonnes opportunités de recherche d'autres inhibiteurs pouissant dans ce domaine. Nous nous sommes intéressés à la synthèse d'analogues du DHAP en diversifiant au maximum les molécules visés. Nous avons tenté en premier lieu de préparer des acides thiohydroxamiques, analogues soufrés des hydroxamates, mais nous avons dû renoncer du fait de leur instabilité. Les tentatives de synthèse de dithiols et de thiirane phosphorylé ont échoué dans les dernières étapes. Nous avons aussi essayé la synthèse d'autres analogues azotés : les amidoximes. Deux ont été préparés : le phospho-glycolo-amidoxime (PGA) et le 3-phosphono-propiono-amidoxime (PPA). De plus, nous avons trouvé une nouvelle voie de synthèse du PGH qui est rapide et économique. Cette stratégie a aussi permis d'obtenir le phospho-glycolo-hydrazide qui n'avait jamais été décrit. Les tests de cinétique enzymatique effectués sur l'aldolase montrent que le PGH (le meilleur inhibiteur existant) est 10 fois plus efficace que le PGA pour l'aldolase de levure et 2 fois pour l'aldolase de muscle de lapin. Le PPA est par contre 1000 fois moins bon que le PGA car il manque pour le fixer au site actif de l'enzyme une liaison hydrogèneThis research work concerns the synthesis of new inhibitors of a not well known enzyme, the class II fructose-1,6-diphosphate aldolase. This enzyme is very interesting as a therapeutic target. The two classes of aldolase have very different ways of processing their substrates and are found in different organisms. The class I can be found everywhere and the class II is only found in microorganisms and mould, including several of pathogenic species. In 1973, phospho-glycolo-hydroxamate (PGH) has been proved to be a very good inhibitor of this enzyme in vitro. It's the only good inhibitor prepared against classe II aldolase. There are still large opportunities of research in this area. We were interessed in the synthesis of several analogs of DHAP. We have first tried to prepare thiohydroxamic acids, as sulfurated analogs of hydroxamates, but these counpounds are not stable enought. Attempts of synthesis of a phosphorylated dithiol and thiirane have failed in the last steps. We also tried the synthesis of another nitrogen containing analogs : amidoximes. Two of them have been prepared : phospho-glycolo-amidoxime (PGA) and 3-phosphono-propiono-amidoxime (PPA). Furthermore, we have found a new fast and cheap way to prepare PGH. The method can also lead to phospho-glycolo-hydrazide which has never been described before. The enzymatic tests carried out on aldolase show that PGA is only 10 times less effective than PGH (best known inhibitor) for yeast aldolase and 2 times for rabbit muscle aldolase. PPA is 1000 times less effective than PGA because of a missing hydrogen bound between an oxygen of phosphate ester and an amino acid of the enzyme
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Guedes-Moali, Catherine. "Etude de l'oxydation et de la reconnaissance d'analogues d'arginine par les no synthases : Synthèse et caracterisation de nouveaux substrats et inhibiteurs." Paris 11, 1999. http://www.theses.fr/1999PA112418.
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Le monoxyde d'azote (NO) est un médiateur biologique essentiel chez les mammifères. Il est produit à partir de la L-arginine par des hémoprotéines appelées NO synthases (NOS). Pour mieux comprendre les conditions de sa production in vivo, nous avons synthétisé une dizaine d'acides aminés contenant les fonctions guanidine, hydroxy-guanidine, amidine ou amidoxime et caractérisé leur capacité à produire des oxydes d'azotes dérivés de NO (nitrite et nitrate) en présence des NOS I et II purifiées. Dans un premier temps, nous avons montré que seulement deux nouveaux composés sont capables de produire NO avec une efficacité comparable à l'arginine (activité monooxygénase). Une plus large gamme de composés à liaison C=NOH peut être transformée en nitrite par les NOS mais dans des proportions environ dix fois plus faibles. La réaction se déroule alors hors du site actif et elle implique l'ion superoxyde produit par l'activité oxydase des NOS. Par là suite, la mesure des constantes d'affinité des acides aminés pour les NOS nous a permis de montrer que deux azotes, positionnés de manière adéquate par rapport à la fonction acide aminé, sont nécessaires pour la reconnaissance et le déclenchement de l'activité monooxygénase. Cette étude nous a également apporté de nombreuses informations sur la façon dont le cofacteur tétrahydrobioptérine contrôle le positionnement du substrat et l'activité des NOS. A partir de ces données, nous avons proposé une nouvelle approche pour la conception d'inhibiteurs de NOSNitric oxide (NO) is a unique biological messenger in mammals. It is produced from L-arginine by hemeproteins called NO synthases (NOS). To get further insight into the mechanism of its biosynthesis, we synthesized a dozen amino-acids bearing a guanidine, hydroxy-guanidine, amidine or amidoxime function and assayed them for their ability to produce nitrogen oxides derived from NO (nitrite and nitrate) in the presence of purified NOS I and II. Thus, we showed that only two new compounds produced NO by a reaction similar to arginine oxidation (monooxygenase activity). A wider set of molecules bearing a C=NOH function were found to be nitrite precursors in the presence of NOS but the reaction proceeded outside the active site, with ten-times lower yields. These compounds were oxidized by the superoxide ion produced by the oxidase activity of NOS. On the other hand, we measured the binding constants of the amino-acids for NOS I and II and demonstrated that two nitrogens, well-positioned relative to the amino-acid moiety, were necessary to allow compounds to bind and be processed by the monooxygenase activity of NOS. Also, this study helped us to understand the role played by the cofactor tetrahydrobiopterin in controlling substrate positioning and NOS activity. These results were used to design new potential inhibitors of NOS
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Kubitza, Christian [Verfasser], Axel [Akademischer Betreuer] Scheidig, and Bernd [Gutachter] Clement. "Structural Characterization of Flavin-dependent Monooxygenases from Zonocerus variegatus and the Human Mitochondrial Amidoxime Reducing Component (mARC) – Enzymes involved in Biotransformation / Christian Kubitza ; Gutachter: Bernd Clement ; Betreuer: Axel Scheidig." Kiel : Universitätsbibliothek Kiel, 2018. http://d-nb.info/1237685664/34.
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Saliba, Rima. "Sorption d'ions métalliques et de colorants sur biopolymères modifiés ou non : application à la dépollution." Lyon 1, 2000. http://www.theses.fr/2000LYO10275.
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JOUSSERANDOT, ANNE. "Coupure oxydante de la double liaison cn des oximes, amidoximes et n-hydroxyguanidines par des cytochromes p450. Comparaison du mecanisme de ces reactions avec celui des no-synthases." Paris 11, 1997. http://www.theses.fr/1997PA112198.
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Le monoxyde d'azote (no), qui joue de multiples roles biologiques, est synthetise en deux etapes a partir de la l-arginine par des enzymes appelees no-synthases (nos). Ces nos sont des hemoproteines ayant de nombreux points communs avec les cytochromes p450. Dans un premier temps, nous avons montre que les p450 hepatiques de rats sont capables d'oxyder des oximes, amidoximes et n-hydroxyguanidines en compose carbonyle correspondant et oxydes d'azote, dont no (mis en evidence par spectroscopie rpe) : reactions analogues a la deuxieme etape de la biosynthese de no par les nos. Les p450 de la famille 3a s'averent etre les plus efficaces pour cette reaction. Les cetoximes, qui font l'objet de la seconde partie, sont metabolisees par deux processus distincts, en cetone et en compose nitre. Les p450 de la famille 3a semblent favoriser la coupure directe en cetone et oxydes d'azote, contrairement aux autres isoformes de p450. Par ailleurs, nous avons mis en evidence l'implication de l'anion superoxyde dans le mecanisme de cette coupure. La troisieme partie traite des amidoximes et des n-hydroxyguanidines. Nous avons mis en evidence, dans certain cas, la formation de compose cyane parallelement au compose carbonyle. Nous avons montre d'autre part que l'anion superoxyde est implique dans le mecanisme de ces deux processus. Il y a donc decouplage du substrat, l'oxydation ayant lieu hors du site actif du p450. L'analogie avec la deuxieme etape de la biosynthese de no par les nos nous a permis de proposer des mecanismes pour l'ensemble de ces reactions.
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Bouhlel, Ahlem. "Cyclisations radicalaires oxydatives médiées par l'acétate de manganèse (III) et orientées vers la chimie médicinale." Thesis, Aix-Marseille, 2012. http://www.theses.fr/2012AIXM5501/document.
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Ce travail s'inscrit dans la recherche et le développement de nouvelles molécules à visée thérapeutique via la mise au point de cyclisations radicalaires oxydatives médiées par l'acétate de manganèse(III). Deux problématiques ont dirigé nos recherches. Tout d'abord, nous avons développé une stratégie de synthèse de prodrogues analogues de la pafuramidine, molécule antileishmanienne. Ainsi, une 1ère série d'amidoximes a été obtenue à partir de β-cétosulfones par une synthèse multi-étapes faisant appel aux réactions i) de cyclisations radicalaires oxydatives médiées par Mn(OAc)3 et ii) de couplages pallado-catalysées de Buchwald-Hartwig et de Heck. Suite à l'évaluation biologique in vitro sur Leishmania donovani et sur des cellules humaines, une 2ème série d'amidoximes et en particulier des monoamidoximes a été réalisée, ce qui a révélé une molécule présentant un index de sélectivité 40 fois plus élevé que celui de la pentamidine, médicament utilisé comme référence. Nous avons également mis au point un double couplage "one-pot" de Buchwald-Hartwig dans le but d'obtenir des produits dicouplés dissymétriques, précurseurs éventuels de futures diamidoximes. Dans une deuxième partie, nous nous sommes focalisés sur la synthèse de composés spirocycliques pouvant constituer un pharmacophore original. De ce fait, une stratégie de synthèse conduisant à divers noyaux tels des tétralines spirocycliques, des spirolactones, des spirobenzophénanthrédin-6(5H)-ones a été mise au point. Ce travail nous a également menés vers la synthèse de dérivés thiobarbiturates, analogues de composés anesthésiques ou anticonvulsivantsThis work focuses on the research and development of new therapeutic molecules through optimized radical cyclizations mediated by manganese(III) acetate. Two problematics directed our research. First, we developed analogous prodrugs of pafuramidine, an antileishmanial molecule. Thus, a 1rst series of amidoximes was obtained from β-ketosulfones by a multi-step synthesis involving i) radical oxidative cyclizations mediated by Mn(OAc)3 and ii) pallado-catalyzed Buchwald-Hartwig and Heck coupling reactions. The 1rst series being biologically evaluated in vitro, both on Leishmania donovani and human cells, a 2nd series and particularly monoamidoximes was prepared and revealed a molecule presenting a selectivity index 40 times higher than the one of pentamidine, used as reference drug compound. We also developed a one-pot double Buchwald-Hartwig coupling reaction in the aim to obtain dissymmetric dicoupled products, potential precursors of future diamidoximes. In a second time, we focused on the synthesis of spirocyclic compounds which could constitute an original pharmacophore. Therefore, we performed a synthesis allowing access to a wide variety of scaffolds such as spirocyclic tetralins, spirolactones, spirobenzophenanthridin-6(5H)-ones. This work allowed the synthesis of thiobarbiturates, analogous of anesthetic or anticonvulsive compounds
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ROH, SOO GYUN. "Synthese et etude structurale de complexes de molybdene (vi) avec des amidoximes fonctionnalisees et de complexes oxo-nitrosyle renfermant le motifm(no)#3#+ ou m(no)#2#2#+ (m = mo, w)." Paris 6, 1994. http://www.theses.fr/1994PA066248.
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Cette these represente une contribution (i) a la chimie de coordination des amidoximes, (ii) a la chimie des complexes oxo-nitrosyles et (iii) a la chimie des polyoxotungstates. Les chapitres i et ii sont consacres a l'etude des reactions de certaines amidoximes fonctionnalisees possedant un groupe thienyle, une fonction alcool ou une fonction amine en ou en b de la fonction amidoxime, vis-a-vis de moo#2(acac)#2 et des polyoxomolybdates. Plusieurs complexes renfermant les motifs moo#4#+, mo#2o#5#2#+, mo#3o#8#2#+, mo#4o#1#1#2#+ mo#4o#1#0(och#3)#2#2#+ et mo#4o#1#2 sont decrits. Le chapitre iii concerne les complexes nitrosyles renfermant le motif mno#4. Le premier exemple de complexe oxo-nitrosyle trinucleaire et de nouveaux composes renfermant un anion mo#5o#1#3(or)#4(no)#3#- stabilise par un cation sodium, oxonium ou amidinium, sont decrits. Ces complexes ont ete obtenus par nitrosylation reductrice de moo#2(acac)#2 ou d'un polyoxomolybdate en presence d'une amidoxime. De plus, la caracterisation des complexes m#5o#1#8m'(no)#3#- (m = w, m' = mo ; m = mo, m' = w) elargit la serie des complexes oxo-nitrosyles derives de la structure de lindqvist. Le chapitre iv decrit les premiers exemples de complexes renfermant un motif m(no)#2#6. La synthese de complexes pentanucleaires renfermant un squelette m#4o#1#2m'(no)#2#2#+m(no)#2#6 (m, m' = mo ou w), comme celle des complexes trinucleaires renfermant un motif mono#4, met a profit la capacite d'assemblage des amidoximes
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Yalala, Bongani Ndhlovu. "Ion exchange resins an functional fibres :a comparative study for the treatment of brine waste water." Thesis, University of the Western Cape, 2009. http://etd.uwc.ac.za/index.php?module=etd&action=viewtitle&id=gen8Srv25Nme4_8342_1298358875.
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To improve the adsorption capacity of polyacrylonitrile (PAN) fibres, hydrophilic amidoxime fibres were prepared by subsequent conversion of the cyano groups to an amidoxime group by reacting with hydroxylamine at 80°
C at an optimum amidoximation time of 2 hrs. The amidoxime fibre was hydrolyzed/alkali treated in a solution of sodium hydroxide to enhance or improve the adsorption properties. This was followed by characterization of the amidoxime and hydrolyzed fibres using Scanning electron microscopy (SEM)
Fourier transform Infrared Spectroscopy (FTIR) and exchange capacity (cationic and anionic). SEM showed that the hydrolysis process made the surface of Amidoxime fibre rougher than that of Polyacrylonitrile fibre. FTIR revealed that the hydrolyzed Amidoxime fibres contained conjugated imine (-C=N-) sequences. Functionalization enhanced the sorption of amidoxime fibres by an increase of 20 % in the cationic exchange capacity. This was achieved by the part conversion of the cyano groups into the carboxylic acid groups. The fibres showed faster kinetics largely due the available exchange sites on the surface of the fibres hence the equilibration was achieved much quicker.
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Gunathilake, Chamila Asanka. "SOFT-TEMPLATING SYNTHESIS OF MESOPOROUS SILICA-BASED MATERIALS FOR ENVIRONMENTAL APPLICATIONS." Kent State University / OhioLINK, 2017. http://rave.ohiolink.edu/etdc/view?acc_num=kent1471543020.
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Lessel, Jürgen. "Amidoxim-Nachbargruppen in Heterocyclensynthesen /." 1988. http://bvbr.bib-bvb.de:8991/F?func=service&doc_library=BVB01&doc_number=001688333&line_number=0001&func_code=DB_RECORDS&service_type=MEDIA.
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謝宗翰. "Synthetic Application of Amidoximes." Thesis, 2013. http://ndltd.ncl.edu.tw/handle/42554511555039820993.
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Hariková, Michaela. "Deriváty amidoximů jako syntetické intermediáty a potenciální léčiva." Master's thesis, 2018. http://www.nusl.cz/ntk/nusl-380440.
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Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Chemistry and Pharmaceutical Analysis Title of diploma thesis: Amidoxime derivatives as synthetic intermediates and potential drugs Student: Michaela Hariková Supervisor: PharmDr. Marta Kučerová, Ph.D. In the theoretical part of this diploma thesis, biological effects of N-hydroxykarbimidoylchlorides and amino derivatives are summarized. In addition, biologically active compounds which are synthesized from N-hydroxykarbimidoylchlorides, in particular the compounds containing isoxazole. In the experimental part, the procedures used for the synthesis of amidoxime derivatives are described. Initial compounds for the synthesis of N-hydroxykarbimidoylchlorides were the corresponding alkylated amidoximes available at the Department of Pharmaceutical Chemistry and Pharmaceutical Analysis or prepared by radical alkylation of pyrazinecarbonitrile followed by conversion to amidoxime. From the N-hydroxykarbimidoylchloride, an amino derivative was subsequently prepared. All prepared compounds were characterized by melting point, NMR and IR spectra. The purity of the substances was checked by TLC and elemental analysis. The prepared derivatives were tested in vitro for their antibacterial, antimycobacterial and antifungal activity.
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Horká, Michaela. "Amidoximy jako syntetické intermediáty a potenciální léčiva I." Master's thesis, 2011. http://www.nusl.cz/ntk/nusl-297218.
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AMIDOXIMES AS SYNTHETIC INTERMEDIATES AND POTENTIAL DRUGS I. Michaela Horká Charles University in Prague, Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Chemistry and Drug Control In the theoretical part of this diploma thesis, biological activities of amidoximes are resumed. They have been studied mainly as prodrugs that are reduced to active compounds - amidines. Some amidoximes reached clinical trials but due to their significant undesirable effects have not been developed further. Methodical part deals with various synthetic procedures for the preparation of amidoximes. In the frame of the experimental part, four 5-alkylpyrazine-2-carbonitriles were synthesized at first. Using hydroxylamine hydrochloride, the nitriles were converted to corresponding amidoximes: N'-hydroxy-5-propylpyrazine-2-carboximidamide N'-hydroxy-5-isopropylpyrazine-2-carboximidamide N'-hydroxy-5-pentylpyrazine-2-carboximidamide N'-hydroxy-5-hexylpyrazine-2-carboximidamide None of the obtained products have been reported yet. They were characterized by melting points, IR, NMR spectra. Their purity was checked by elemental analysis. The compounds were tested for antifungal and antibacterial activity but were found non-effective. This is probably due to the fact that in vitro their bioactivation...
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Oravcová, Dominika. "Amidoximy jako syntetické intermediáty a potenciální léčiva II." Master's thesis, 2017. http://www.nusl.cz/ntk/nusl-368027.
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Diploma thesis Charles University Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Chemistry and Pharmaceutical Analysis Student: Dominika Oravcová Supervisor: PharmDr. Marta Kučerová, Ph.D. Title of the thesis: Amidoximes as synthetic intermediates and potential drugs II. Diploma thesis is focused on amidoxime derivates, specifically their esters. In the theoretical part, biological activities of amidoxime esters are described, particularly their antibacterial and antiprotozoal activity. Experimental part contains preparation of seven amidoxime esters. The syntheses afforded three N'-acetoxypyrazine-2-carboximidamides and four N'-pivaloyloxypyrazine-2-carboximidamides. Products prepared in this thesis have not yet been described in any literature. All prepared esters were characterized by their melting points and spectra - IR and NMR. Purity of these compounds was confirmed by elemental analysis. Biological activity of these esters was also tested, to check their antibacterial and antifungal abilities. Four substances showed mild activity against M. tuberculosis. Other biological tests did not show any activity.
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Lopian, Katrin. "Enzymatische Grundlagen der Aktivierung des Amidoxim- und Ester-Prodrugs Ximelagatran /." 2002. http://www.gbv.de/dms/bs/toc/356907805.pdf.
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Harsdorf, Angela. "In vitro Biotransformationsstudien von N-Hydroxyguanidinen und Amidoximen /." 1998. http://www.gbv.de/dms/bs/toc/251187489.pdf.
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Katirtzi, Anastasia. "Amidoximes as intermediates for the synthesis of potential drugs." Master's thesis, 2015. http://www.nusl.cz/ntk/nusl-332856.
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Charles University in Prague, Faculty of Pharmacy in Hradec Králové Department of Pharmaceutical Chemistry and Pharmaceutical Analysis Student: Anastasia Katirtzi Supervisor: Assoc. Prof. RNDr. Veronika Opletalová, Ph.D. Title of Diploma Thesis: Amidoximes as intermediates for the synthesis of potential drugs The current thesis is focused on the O-acylation of pyrazine amidoximes and their cyclization to the corresponding 3,5-disubstituted- 1,2,4-oxadiazoles. 5-unsubstituted and 5-butylpyrazine amidoximes were acylated by acetic anhydride, trimethylacetic anhydride and 2,3-pyrazinecarboxylic anhydride as acylating agents in toluene. Formation of oxadiazoles was achieved in xylene, using acetic anhydride for acylation. Identification of the products was done by melting points, NMR and IR spectra, and their purity was proved by elemental analysis Furthermore, amidoximes and their derivatives were subjected to biological assay in order to evaluate their in vitro antifungal and antibacterial properties. Unfortunatelly, amidoximes and 1,2,4-oxadiazoles were inactive. For the esters, biological results will be available later.
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Lindner, Harry Dreyfus. "A cost estimate for uranium recovery from seawater using a chitin nanomat adsorbent." Thesis, 2014. http://hdl.handle.net/2152/26323.
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Even at 3.3 ppb, seawater contains a uranium supply large enough to power the world’s nuclear fleet for 13,000 years. This large supply has prompted interest in technologies for recovering uranium from seawater. Since the 1960’s, economic models of such technologies have failed to produce an economically competitive strategy when compared to conventional uranium recovery from terrestrial mining. Thus, uranium from seawater is researched as a potential price ceiling because of the large supply but high recovery cost. Such an upper bound is still valuable research because it allows for more certainty in uranium prices for planning, research, development and deployment of nuclear power systems. This thesis explores past cost estimates for uranium recovery from seawater and adds a new cost estimate to the pool of literature.
The past estimates showed a development from systems that actively moved seawater to systems that allowed adsorbent to sit passively in seawater. The adsorbent material changed from hydrous titanium oxide to the higher-capacity amidoxime ligand. Capacity was the strongest driver of cost. Early models with the amidoxime ligand used an acrylic substrate or backbone. This substrate was later replaced by polyethylene because of its increased durability and lower cost. However, each of those materials could contribute to the problem of plastics in the ocean.
The new technology assessed for cost in this paper attempts to address the plastics concern by replacing the plastic with a high molecular weight chitin nanomat as the substrate for the amidoxime ligand. The cost assessment showed the technology is presently cost prohibitive largely due to the adsorption capacity and chitin nanomat production costs. To increase capacity, the grafting efficiency onto the chitin substrate must be improved in order to achieve capacities comparable to those observed for the amidoxime-polyethylene adsorbent. To reduce chitin nanomat production costs, the ionic liquid (IL) consumption must be reduced and the recyclability of IL must be achieved.text
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廖本原. "(1) Synthetic Studies of Benzimidazoles from Amidoximes (2) Copper-Catalyzed Synthesis of Indoles." Thesis, 2014. http://ndltd.ncl.edu.tw/handle/04716447104067185921.
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碩士國立臺灣師範大學
化學系
102
This thesis covers two separated topics. The first part is the synthesis of N-phenyl hetero-aryl carboxamidoximes with different substituents on the bezene ring. The reaction of the N-phenyl hetero-aryl carboxamidoximes with p-toluenesulfonic anhydride undergoes a direct intramolecular electrophilic aromatic substitution at low temperature, to afford 2-hetero-arylbenzimidazole derivatives. Moreover, we also found that the reaction of arylcarboxamidoximes with different sulfonyl reagents undergo Tiemann rearrangement reaction to afford corresponding of N,N’-disubstituted ureas. The second part focuses on studying the synthesis of 3-cyanoindole derivatives. N-(o- ethynylphenyl)- N-tosylcyanamide derivatives were prepared from corresponding o-haloanilines or o-halobenzonitrile. 3-Cyanoindole derivatives were obtained when treatment of o-ethynylphenyl cyanamides with a catalytic amount of CuI.