Academic literature on the topic 'Amidoxima'

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Journal articles on the topic "Amidoxima"

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Coutinho, Fernanda M. B., Simone M. Rezende, and Celina C. R. Barbosa. "Resinas quelantes amidoxímicas." Polímeros 9, no. 4 (December 1999): 129–35. http://dx.doi.org/10.1590/s0104-14281999000400022.

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Resinas quelantes com grupos amidoxima foram sintetizadas por copolimerização em suspensão de acrilonitrila (AN) e divinilbenzeno (DVB) e subsequente modificação química dos grupos ciano por reação com hidroxilamina. Na copolimerização, a proporção de divinilbenzeno e o grau de diluição foram variados. Gelatina e carbonato de cálcio foram usados como estabilizadores de suspensão e sulfato de sódio foi adicionado para reduzir a solubilidade da acrilonitrila em água, por meio do efeito salting out. Os copolímeros de AN/DVB e as resinas amidoxímicas obtidos foram caracterizados por meio de densidade aparente, área específica, volume de poros e teor de nitrogênio. As resinas amidoxímicas foram também avaliadas em relação a capacidade de complexação de íons cobre.
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Decato, Daniel A., and Orion B. Berryman. "Structural and computational characterization of a bridging zwitterionic-amidoxime uranyl complex." Organic Chemistry Frontiers 6, no. 7 (2019): 1038–43. http://dx.doi.org/10.1039/c9qo00267g.

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Zhang, Linjuan, Meiying Qie, Jing Su, Shuo Zhang, Jing Zhou, Jiong Li, Yu Wang, et al. "Tris-amidoximate uranyl complexesviaη2binding mode coordinated in aqueous solution shown by X-ray absorption spectroscopy and density functional theory methods." Journal of Synchrotron Radiation 25, no. 2 (February 19, 2018): 514–22. http://dx.doi.org/10.1107/s160057751800067x.

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The present study sheds some light on the long-standing debate concerning the coordination properties between uranyl ions and the amidoxime ligand, which is a key ingredient for achieving efficient extraction of uranium. Using X-ray absorption fine structure combined with theoretical simulation methods, the binding mode and bonding nature of a uranyl–amidoxime complex in aqueous solution were determined for the first time. The results show that in a highly concentrated amidoxime solution the preferred binding mode between UO22+and the amidoxime ligand is η2coordination with tris-amidoximate species. In such a uranyl–amidoximate complex with η2binding motif, strong covalent interaction and orbital hybridization between U 5f/6dand (N, O) 2pshould be responsible for the excellent binding ability of the amidoximate ligand to uranyl. The study was performed directly in aqueous solution to avoid the possible binding mode differences caused by crystallization of a single-crystal sample. This work also is an example of the simultaneous study of local structure and electronic structure in solution systems using combined diagnostic tools.
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Al-Mousawi, Saleh Mohammed, Moustafa Sherief Moustafa, and Mohamed Hilmy Elnagdi. "Studies with 2-Arylhydrazononitriles: Further Investigations on the Utility of 2-Arylhydrazononitriles as Precursors to 1,2,3-Triazole Amines." Journal of Chemical Research 2007, no. 9 (September 2007): 515–18. http://dx.doi.org/10.3184/030823407x244869.

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3-Oxo-2-arylhydrazonobutanenitriles react with hydroxylamine hydrochloride in ethanolic sodium acetate to yield either amidoximes or isoxazolamines depending on the nature of the substituent. The amidoximes cyclise in refluxing DMF containing piperidine to form 2-aryl-1,2,3-triazol-5-amines. The isoxazolamines rearranged into 1,2,3-triazolamines on refluxing in DMF. Amidoxime 2c cyclised in acetic anhydride to give 2-arylhydrazono-1,2,4-oxadiazole 9c, which rearranged to acetylamino-1,2,3-triazole 8c. The prepared acetyl-1,2,3-triazolamines 8b,c were utilised as precursors to triazolopyridines and pyrazolyltriazoles.
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Hall, James Edwin, John E. Kerrigan, Kishore Ramachandran, Brendan C. Bender, Jason P. Stanko, Susan K. Jones, Donald A. Patrick, and Richard R. Tidwell. "Anti-Pneumocystis Activities of Aromatic Diamidoxime Prodrugs." Antimicrobial Agents and Chemotherapy 42, no. 3 (March 1, 1998): 666–74. http://dx.doi.org/10.1128/aac.42.3.666.

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ABSTRACT Aromatic dicationic compounds, such as pentamidine, have potent antimicrobial activities. Clinical use of these compounds has been restricted, however, by their toxicity and limited oral activity. A novel approach, using amidoxime derivatives as prodrugs, has recently been proposed to overcome these limitations. Although results were presented for amidoxime derivatives of only one diamidine, pentamidine, the authors in the original proposal claimed that amidoxime derivatives would work as effective prodrugs for all pharmacologically active diamidines. Nine novel amidoxime derivatives were synthesized and tested in the present study for activity against Pneumocystis carinii in corticosteroid-suppressed rats. Only three of the nine compounds had significant oral anti-Pneumocystis activity. The bisbenzamidoxime derivatives of three direct pentamidine analogs had excellent oral and intravenous activities and reduced acute host toxicity. These compounds are not likely candidates for future drug development, however, because they have chronic toxic effects and the active amidine compounds have multiple sites susceptible to oxidative metabolism, which complicates their pharmacology and toxicology. Novel diamidoximes from three other structural classes, containing different groups linking the cationic moieties, lacked significant oral or intravenous anti-Pneumocystis activity, even though the corresponding diamidines were very active intravenously. Both active and inactive amidoximes were readily metabolized to the corresponding amidines by cell-free liver homogenates. Thus, the amidoxime prodrug approach may provide a strategy to exploit the potent antimicrobial and other pharmacological activities of selected, but certainly not all, aromatic diamidines.
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Medeiros, Herbert Igor Rodrigues de, Bruna Barbosa Maia da Silva, Carlos Eduardo Rodrigues Aguiar, Thiago Araújo de Medeiros Brito, Fernando Emanuel de Sousa Ferreira, Natan Dias Fernandes, Érika Paiva de Moura, and Francisco Cesino de Medeiros Júnior. "SÍNTESE, ELUCIDAÇÃO DA ARQUITETURA MOLECULAR E AVALIAÇÃO DO POTENCIAL CITOTÓXICO DE UM PROMISSOR CANDIDATO A FÁRMACO DERIVADO DE AMIDOXIMA / SYNTHESIS, ELUCIDATION OF MOLECULAR ARCHITECTURE AND EVALUATION OF THE CYTOTOXIC POTENTIAL OF A PROMISING DRUG CANDIDATE DERIVED FROM AMIDOXIME." Brazilian Journal of Development 6, no. 9 (2020): 66070–79. http://dx.doi.org/10.34117/bjdv6n9-149.

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Md Jamil, Siti Nurul Ain, Mastura Khairuddin, and Rusli Daik. "Preparation of acrylonitrile/acrylamide copolymer beads via a redox method and their adsorption properties after chemical modification." e-Polymers 15, no. 1 (January 1, 2015): 45–54. http://dx.doi.org/10.1515/epoly-2014-0109.

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AbstractPoly(acrylonitrile-co-acrylamide) [poly(AN-co- AM)] was prepared via a redox method, with sodium bisulfite and potassium persulphate as the initiators. High yield was attained in up to 76% of monomer conversion within 3 h of reaction time. The copolymers were then chemically modified with hydroxylamine hydrochloride to obtain amidoxime functional groups in the polyacrylonitrile (PAN) system. The role of the amidoxime group is to form a chelating ion-exchange network based on acrylonitrile for the adsorption of heavy metal ions in aqueous solution. Based on the Fourier transform infrared spectra, the appearance of a strong band at the regions of 1680 and 3300–3400 cm-1 due to the stretching vibration of C=O and NH2 groups, respectively, confirmed the copolymerization of acrylamide into the PAN system. In the case of modified copolymers, there was an appearance of broad bands at the regions of ∼3300 and ∼900 cm-1, which corresponded to the stretching vibrations of O-H and =N-O, respectively, from the oxime group. The scanning electron microscopy showed that the average size of the copolymer particles was ∼149 nm, and the average size increased to ∼217 nm in the case of the modified copolymer. The amidoximed poly(AN-co-AM) was analyzed by inductively coupled plasma to investigate its adsorption behavior toward Cu(II).
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MOURA, A. L., J. F. SILVA, J. J. R. DE FREITAS, J. C. R. FREITAS, and J. R. DE FREITAS FILHO. "EXPERIENCING A SYNTHESIS ONE-POT OF 1,2,4-OXADIAZOLE MEDIATED BY MICROWAVE OVEN: GREEN CHEMISTRY IN FOCUS." Periódico Tchê Química 16, no. 32 (August 20, 2019): 820–32. http://dx.doi.org/10.52571/ptq.v16.n32.2019.838_periodico32_pgs_820_832.pdf.

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1,2,4-oxadiazoles are compounds that have attracted the attention of many researchers due to their wide range of biological activities, for example, anti-inflammatory, antimicrobial, antitumor etc. The syntheses are based mostly on the use of amidoximes and acylating agents as the initial reactants. This work aims to describe a one-pot reaction for the synthesis of 1,2,4-oxadiazols, mediated by microwave irradiation, employing home-use microwave oven, in the discipline of heterocyclic Chemistry in the postgraduate. The methodology consisted of the reaction of nitriles, hydroxylamine hydrochloride, potassium carbonate and different esters to obtain 1,2,4-oxadiazole. The reactions include two sequential procedures: base-promoted intermolecular addition of hydroxylamine to nitrile to lead to amidoxime, then treatment of the amidoxime with esther to form 1,2,4-oxadiazoles in good yields. This method represents a direct and simple protocol for the synthesis of 3,5-disubstituted 1,2,4-oxadiazoles. It was initially discussed with the students the chemistry of the oxadiazoles, one-pot reactions and green chemistry through atheoretical-expository-dialogue strategy. In the course of the didactic intervention the students, through a thematic seminary, presented the results of the analysis of the spectra from the different techniques used. With the skills acquired from completing this laboratory work, the students become well-prepared to perform spectroscopic analyzes in subsequent experiments encountered in the organic chemistry laboratory.
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Möhrle, Hans, Karin Bluhme-Hensen, Birgit Middelhauve, Dietrich Mootz, and Hartmut Wunderlich. "Cyclisierung von Amidoximen mit Oxybis(diphenylboran) / Cyclization of Amidoximes with Oxybis(diphenylborane)." Zeitschrift für Naturforschung B 46, no. 9 (September 1, 1991): 1219–22. http://dx.doi.org/10.1515/znb-1991-0914.

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Substituted amidoximes when reacted with oxybis(diphenylborane) do not yield ester chelates as main products but boron heterocycles. The compound obtained from p-toluamidoxime was found by crystal structure analysis to be 2-phenyl-4-(4-methylphenyl)-2,3-dihydro-1,3,5,2-oxadiazaborol (9). The conformation of the molecule is determined by angles of 29.1 and 24.4° between the planes of adjacent rings. Except N–O all bonds in the heterocyclic ring contain significant π character. Molecules are linked to chains by a weak bifurcated hydrogen bond. 9 crystallizes with the monoclinic space group P21/c, Ζ = 4, a = 5.574(2), b = 18.274(4), c = 12.754(4) Å, β = 106.41(2)°. Refinement of 227 parameters using 1709 observed reflections converged at R = 0.037.
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Markov, Andrey V., Aleksandra V. Sen’kova, Irina I. Popadyuk, Oksana V. Salomatina, Evgeniya B. Logashenko, Nina I. Komarova, Anna A. Ilyina, Nariman F. Salakhutdinov, and Marina A. Zenkova. "Novel 3′-Substituted-1′,2′,4′-Oxadiazole Derivatives of 18βH-Glycyrrhetinic Acid and Their O-Acylated Amidoximes: Synthesis and Evaluation of Antitumor and Anti-Inflammatory Potential In Vitro and In Vivo." International Journal of Molecular Sciences 21, no. 10 (May 15, 2020): 3511. http://dx.doi.org/10.3390/ijms21103511.

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A series of novel 18βH-glycyrrhetinic acid (GA) derivatives containing 3′-(alkyl/phenyl/pyridin(-2″, -3″, and -4″)-yl)-1′,2′,4′-oxadiazole moieties at the C-30 position were synthesized by condensation of triterpenoid’s carboxyl group with corresponding amidoximes and further cyclization. Screening of the cytotoxicity of novel GA derivatives on a panel of tumor cell lines showed that the 3-acetoxy triterpenoid intermediates—O-acylated amidoxime 3a-h—display better solubility under bioassay conditions and more pronounced cytotoxicity compared to their 1′,2′,4′-oxadiazole analogs 4f-h (median IC50 = 7.0 and 49.7 µM, respectively). Subsequent replacement of the 3-acetoxy group by the hydroxyl group of pyridin(-2″, 3″, and -4″)-yl-1′,2′,4′-oxadiazole-bearing GA derivatives produced compounds 5f-h, showing the most pronounced selective toxicity toward tumor cells (median selectivity index (SI) > 12.1). Further detailed analysis of the antitumor activity of hit derivative 5f revealed its marked proapoptotic activity and inhibitory effects on clonogenicity and motility of HeLa cervical carcinoma cells in vitro, and the metastatic growth of B16 melanoma in vivo. Additionally, the comprehensive in silico study revealed intermediate 3d, bearing the tert-butyl moiety in O-acylated amidoxime, as a potent anti-inflammatory candidate, which was able to effectively inhibit inflammatory response induced by IFNγ in macrophages in vitro and carrageenan in murine models in vivo, probably by primary interactions with active sites of MMP9, neutrophil elastase, and thrombin. Taken together, our findings provide a basis for a better understanding of the structure–activity relationship of 1′,2′,4′-oxadiazole-containing triterpenoids and reveal two hit molecules with pronounced antitumor (5f) and anti-inflammatory (3d) activities.
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Dissertations / Theses on the topic "Amidoxima"

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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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Coordenação de Aperfeiçoamento de Pessoal de Nível Superior - CAPES
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 référence
Leishmaniasis 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 évaluées
Amidoxime 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 étude
This 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 pentamidoxime
The 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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Abstract:
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 orale
The 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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Book chapters on the topic "Amidoxima"

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Jarvis, Neldon L., John Lint, Arthur W. Snow, and Hank Wohltjen. "Amidoxime-Functionalized Coatings for Surface Acoustic Wave Detection of Simulant Vapors." In ACS Symposium Series, 309–19. Washington, DC: American Chemical Society, 1986. http://dx.doi.org/10.1021/bk-1986-0309.ch018.

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Ostrowska, K., and A. Kolasa. "Reduction of Amidoximes." In Three Carbon-Heteroatom Bonds: Amides and Derivatives; Peptides; Lactams, 1. Georg Thieme Verlag KG, 2005. http://dx.doi.org/10.1055/sos-sd-022-00551.

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Hemming, K. "From -(Dicyanovinyl)amidoximes." In Five-Membered Hetarenes with Three or More Heteroatoms, 1. Georg Thieme Verlag KG, 2004. http://dx.doi.org/10.1055/sos-sd-013-00215.

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Wilkins, D. J., and P. A. Bradley. "Amidoximes and Isothiocyanates." In Five-Membered Hetarenes with Three or More Heteroatoms, 1. Georg Thieme Verlag KG, 2004. http://dx.doi.org/10.1055/sos-sd-013-00430.

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Hemming, K. "From an Amidoxime and Phosgene." In Five-Membered Hetarenes with Three or More Heteroatoms, 1. Georg Thieme Verlag KG, 2004. http://dx.doi.org/10.1055/sos-sd-013-00193.

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Ostrowska, K., and A. Kolasa. "Amidoximes (N-Hydroxylated Amidines)." In Three Carbon-Heteroatom Bonds: Amides and Derivatives; Peptides; Lactams, 1. Georg Thieme Verlag KG, 2005. http://dx.doi.org/10.1055/sos-sd-022-00575.

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Braverman, S., M. Cherkinsky, and M. L. Birsa. "Tiemann Rearrangements of Amidoximes." In Four Carbon-Heteroatom Bonds, 1. Georg Thieme Verlag KG, 2005. http://dx.doi.org/10.1055/sos-sd-018-00314.

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Hemming, K. "From an Amidoxime and a Chloroformate." In Five-Membered Hetarenes with Three or More Heteroatoms, 1. Georg Thieme Verlag KG, 2004. http://dx.doi.org/10.1055/sos-sd-013-00192.

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Hemming, K. "From an Amidoxime and an Anhydride." In Five-Membered Hetarenes with Three or More Heteroatoms, 1. Georg Thieme Verlag KG, 2004. http://dx.doi.org/10.1055/sos-sd-013-00197.

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Hemming, K. "From an Amidoxime and a Cyanate." In Five-Membered Hetarenes with Three or More Heteroatoms, 1. Georg Thieme Verlag KG, 2004. http://dx.doi.org/10.1055/sos-sd-013-00201.

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Conference papers on the topic "Amidoxima"

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Wei, Guilin, Fangting Chi, Pinglin Guo, Ziyue Gong, Fule Liu, and Tianli Qiu. "Amidoxime Selective Adsorption for Uranyl and Transition Metals." In 2015 International Symposium on Energy Science and Chemical Engineering. Paris, France: Atlantis Press, 2015. http://dx.doi.org/10.2991/isesce-15.2015.29.

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Tang, Wen-Ling, Lei Xie, Hui-Juan Wang, and Sai Wang. "Removal of Pb by Adsorption of Amidoxime Group Modified Carbon Nanotubes." In 2015 International Conference on Material Science and Applications (icmsa-15). Paris, France: Atlantis Press, 2015. http://dx.doi.org/10.2991/icmsa-15.2015.128.

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Abdullah, M., R. A. Majid, L. C. Abdullah, M. F. Abdul-Wahab, M. Q. F. A. Aziz, N. H. M. Sabri, S. A. Hamdan, S. N. A. Zaiton, and S. H. A. Muhamad. "Functionalization of polyacrylonitrile-grafted cellulose with amidoxime and its antimicrobial property." In 4TH ELECTRONIC AND GREEN MATERIALS INTERNATIONAL CONFERENCE 2018 (EGM 2018). Author(s), 2018. http://dx.doi.org/10.1063/1.5080855.

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Wang, Jihua. "Adsorption behavior of Zn (II) from amidoxime functionalized mesoporous silica SBA-15." In 2016 5th International Conference on Environment, Materials, Chemistry and Power Electronics. Paris, France: Atlantis Press, 2016. http://dx.doi.org/10.2991/emcpe-16.2016.55.

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Reports on the topic "Amidoxima"

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Kuo, Li-Jung, Gary A. Gill, Jonathan E. Strivens, Jordana R. Wood, Nicholas J. Schlafer, Chien M. Wai, and H. B. Pan. Investigations Into the Reusability of Amidoxime-Based Polymeric Uranium Adsorbents. Office of Scientific and Technical Information (OSTI), September 2016. http://dx.doi.org/10.2172/1330925.

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Yiacoumi, Sotira, and Costas Tsouris. Optimizing Polymer-Grafted Amidoxime-based Adsorbents for Uranium Uptake from Seawater. Office of Scientific and Technical Information (OSTI), January 2019. http://dx.doi.org/10.2172/1491738.

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Gill, Gary A., Li-Jung Kuo, Jonathan E. Strivens, Jordana R. Wood, Chien Wai, and Horng-Bin Pan. Investigations into Alternative Desorption Agents for Amidoxime-Based Polymeric Uranium Adsorbents. Office of Scientific and Technical Information (OSTI), June 2015. http://dx.doi.org/10.2172/1322540.

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Rogers, Robin Don, and Gabriela Gurau. Understanding the Interactions of Seawater Ions with Amidoxime through X-Ray Crystallography. Office of Scientific and Technical Information (OSTI), December 2019. http://dx.doi.org/10.2172/1580560.

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Wai, Chien M. Innovative Elution Processes for Recovering Uranium and Transition Metals from Amidoxime-based Adsorbents. Office of Scientific and Technical Information (OSTI), April 2017. http://dx.doi.org/10.2172/1351974.

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Jiang, De-en. Quantitative Prediction of Uranium Speciation and Amidoxime Binding in Seawater from Advanced Simulation Techniques. Office of Scientific and Technical Information (OSTI), December 2018. http://dx.doi.org/10.2172/1490188.

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Gill, Gary A., Li-Jung Kuo, Jonathan E. Strivens, Jordana R. Wood, Nicholas J. Schlafer, Costas Tsouris, Austin Ladshaw, and Sotira Yiacoumi. Investigations into the Effect of Current Velocity on Amidoxime-Based Polymeric Uranium Adsorbent Performance. Office of Scientific and Technical Information (OSTI), December 2015. http://dx.doi.org/10.2172/1332628.

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Gill, Gary A., Li-Jung Kuo, Jonathan E. Strivens, Jiyeon Park, George T. Bonheyo, Robert T. Jeters, Nicholas J. Schlafer, and Jordana R. Wood. Determination of Adsorption Capacity and Kinetics of Amidoxime-Based Uranium Adsorbent Braided Material in Unfiltered Seawater Using a Flume Exposure System. Office of Scientific and Technical Information (OSTI), August 2015. http://dx.doi.org/10.2172/1332627.

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Gill, Gary A., Li-Jung Kuo, Jonathan E. Strivens, Jordana R. Wood, Nicholas J. Schlafer, Christopher J. Janke, Sadananda Das, et al. Summary of Adsorption Capacity and Adsorption Kinetics of Uranium and Other Elements on Amidoxime-based Adsorbents from Time Series Marine Testing at the Pacific Northwest National Laboratory. Office of Scientific and Technical Information (OSTI), September 2016. http://dx.doi.org/10.2172/1330924.

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