The Experts below are selected from a list of 14910 Experts worldwide ranked by ideXlab platform
Robin E B Lee - One of the best experts on this subject based on the ideXlab platform.
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synthesis and evaluation of cyclic Secondary Amine substituted phenyl and benzyl nitrofuranyl amides as novel antituberculosis agents
Journal of Medicinal Chemistry, 2005Co-Authors: Rajendra P Tangallapally, Raghunandan Yendapally, And Anne J M Lenaerts, Robin E B LeeAbstract:In an ongoing effort to develop new and potent antituberculosis agents, a second-generation series of nitrofuranyl amides was synthesized on the basis of the lead compound 5-nitrofuran-2-carboxylic acid 3,4-dimethoxybenzylamide. The primary design consideration was to improve the solubility and consequently the bioavailability of the series by the addition of hydrophilic rings to the benzyl and phenyl B ring core. The synthesis of 27 cyclic, Secondary Amine substituted phenyl and benzyl nitrofuranyl amides is described and their activity against Mycobacterium tuberculosis reported. The series showed a strong structure-activity relationship as the benzyl nitrofuranyl amides were significantly more active than similarly substituted phenyl nitrofuranyl amides. Para-substituted benzyl piperazines showed the most antituberculosis activity. Compounds in the series were subsequently selected for bioavailability and in vivo testing. This study led to the successful discovery of novel compounds with increased antituberculosis activity in vitro and a better understanding of the requisite pharmacological properties to advance this class.
And Anne J M Lenaerts - One of the best experts on this subject based on the ideXlab platform.
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synthesis and evaluation of cyclic Secondary Amine substituted phenyl and benzyl nitrofuranyl amides as novel antituberculosis agents
Journal of Medicinal Chemistry, 2005Co-Authors: Rajendra P Tangallapally, Raghunandan Yendapally, And Anne J M LenaertsAbstract:In an ongoing effort to develop new and potent antituberculosis agents, a second-generation series of nitrofuranyl amides was synthesized on the basis of the lead compound 5-nitrofuran-2-carboxylic acid 3,4-dimethoxybenzylamide. The primary design consideration was to improve the solubility and consequently the bioavailability of the series by the addition of hydrophilic rings to the benzyl and phenyl B ring core. The synthesis of 27 cyclic, Secondary Amine substituted phenyl and benzyl nitrofuranyl amides is described and their activity against Mycobacterium tuberculosis reported. The series showed a strong structure−activity relationship as the benzyl nitrofuranyl amides were significantly more active than similarly substituted phenyl nitrofuranyl amides. Para-substituted benzyl piperazines showed the most antituberculosis activity. Compounds in the series were subsequently selected for bioavailability and in vivo testing. This study led to the successful discovery of novel compounds with increased anti...
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synthesis and evaluation of cyclic Secondary Amine substituted phenyl and benzyl nitrofuranyl amides as novel antituberculosis agents
Journal of Medicinal Chemistry, 2005Co-Authors: Rajendra P Tangallapally, Raghunandan Yendapally, And Anne J M Lenaerts, Robin E B LeeAbstract:In an ongoing effort to develop new and potent antituberculosis agents, a second-generation series of nitrofuranyl amides was synthesized on the basis of the lead compound 5-nitrofuran-2-carboxylic acid 3,4-dimethoxybenzylamide. The primary design consideration was to improve the solubility and consequently the bioavailability of the series by the addition of hydrophilic rings to the benzyl and phenyl B ring core. The synthesis of 27 cyclic, Secondary Amine substituted phenyl and benzyl nitrofuranyl amides is described and their activity against Mycobacterium tuberculosis reported. The series showed a strong structure-activity relationship as the benzyl nitrofuranyl amides were significantly more active than similarly substituted phenyl nitrofuranyl amides. Para-substituted benzyl piperazines showed the most antituberculosis activity. Compounds in the series were subsequently selected for bioavailability and in vivo testing. This study led to the successful discovery of novel compounds with increased antituberculosis activity in vitro and a better understanding of the requisite pharmacological properties to advance this class.
Rajendra P Tangallapally - One of the best experts on this subject based on the ideXlab platform.
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synthesis and evaluation of cyclic Secondary Amine substituted phenyl and benzyl nitrofuranyl amides as novel antituberculosis agents
Journal of Medicinal Chemistry, 2005Co-Authors: Rajendra P Tangallapally, Raghunandan Yendapally, And Anne J M LenaertsAbstract:In an ongoing effort to develop new and potent antituberculosis agents, a second-generation series of nitrofuranyl amides was synthesized on the basis of the lead compound 5-nitrofuran-2-carboxylic acid 3,4-dimethoxybenzylamide. The primary design consideration was to improve the solubility and consequently the bioavailability of the series by the addition of hydrophilic rings to the benzyl and phenyl B ring core. The synthesis of 27 cyclic, Secondary Amine substituted phenyl and benzyl nitrofuranyl amides is described and their activity against Mycobacterium tuberculosis reported. The series showed a strong structure−activity relationship as the benzyl nitrofuranyl amides were significantly more active than similarly substituted phenyl nitrofuranyl amides. Para-substituted benzyl piperazines showed the most antituberculosis activity. Compounds in the series were subsequently selected for bioavailability and in vivo testing. This study led to the successful discovery of novel compounds with increased anti...
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synthesis and evaluation of cyclic Secondary Amine substituted phenyl and benzyl nitrofuranyl amides as novel antituberculosis agents
Journal of Medicinal Chemistry, 2005Co-Authors: Rajendra P Tangallapally, Raghunandan Yendapally, And Anne J M Lenaerts, Robin E B LeeAbstract:In an ongoing effort to develop new and potent antituberculosis agents, a second-generation series of nitrofuranyl amides was synthesized on the basis of the lead compound 5-nitrofuran-2-carboxylic acid 3,4-dimethoxybenzylamide. The primary design consideration was to improve the solubility and consequently the bioavailability of the series by the addition of hydrophilic rings to the benzyl and phenyl B ring core. The synthesis of 27 cyclic, Secondary Amine substituted phenyl and benzyl nitrofuranyl amides is described and their activity against Mycobacterium tuberculosis reported. The series showed a strong structure-activity relationship as the benzyl nitrofuranyl amides were significantly more active than similarly substituted phenyl nitrofuranyl amides. Para-substituted benzyl piperazines showed the most antituberculosis activity. Compounds in the series were subsequently selected for bioavailability and in vivo testing. This study led to the successful discovery of novel compounds with increased antituberculosis activity in vitro and a better understanding of the requisite pharmacological properties to advance this class.
Keiji Maruoka - One of the best experts on this subject based on the ideXlab platform.
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regio and stereoselective conjugate addition of aldehydes to β tosyl enones under the catalysis of a binaphthyl modified chiral Amine
ChemInform, 2015Co-Authors: Taichi Kano, Hisashi Sugimoto, Hiroki Maruyama, Keiji MaruokaAbstract:The regio-, diastereo-, and enantioselective addition of aliphatic aldehydes to β-tosyl enones is achieved in the presence of axially chiral binaphthyl based Secondary Amine catalysts.
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unusual anti selective asymmetric conjugate addition of aldehydes to nitroalkenes catalyzed by a biphenyl based chiral Secondary Amine
Chemical Communications, 2013Co-Authors: Taichi Kano, Hisashi Sugimoto, Osamu Tokuda, Keiji MaruokaAbstract:Unusual anti-selectivity was observed in the conjugate addition of aldehydes to nitroalkenes, when a biphenyl-based chiral Secondary Amine was used as catalyst.
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unique properties of chiral biaryl based Secondary Amine catalysts for asymmetric enAmine catalysis
Chemical Science, 2013Co-Authors: Taichi Kano, Keiji MaruokaAbstract:A series of biaryl-based Secondary Amine catalysts with various functional groups have been designed as new chiral Amine catalysts. These chiral organocatalysts have been successfully applied to several asymmetric reactions via enAmine intermediates and exhibited unique reactivity and selectivity in comparison with proline and its derivatives.
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direct asymmetric bromination of aldehydes catalyzed by a binaphthyl based Secondary Amine highly enantio and diastereoselective one pot synthesis of bromohydrins
Chemical Communications, 2010Co-Authors: Taichi Kano, Fumitaka Shirozu, Keiji MaruokaAbstract:One-pot stereoselective synthesis of bromohydrins as a useful chiral building block was achieved by the reaction of Grignard reagents with optically active α-bromoaldehydes, which were in situ generated by direct asymmetric bromination of aldehydes catalyzed by a binaphthyl-based Secondary Amine (S)-3.
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design of chiral bifunctional Secondary Amine catalysts for asymmetric enAmine catalysis
ChemInform, 2009Co-Authors: Taichi Kano, Keiji MaruokaAbstract:A series of binaphthyl-based Secondary Amine catalysts containing various functional groups have been designed as new chiral bifunctional Amine catalysts. These chiral organocatalysts have been successfully applied to several asymmetric reactions via enAmine intermediates and exhibit unique reactivity and selectivity in comparison with proline and its derivatives.
D L Massart - One of the best experts on this subject based on the ideXlab platform.
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development of a generic flow injection analysis method for compounds with a Secondary Amine or amide function using an experimental design approach part ii selection and evaluation of the chemical reaction parameters
Analytica Chimica Acta, 2002Co-Authors: C Vannecke, M S Bloomfield, Vander Y Heyden, D L MassartAbstract:Abstract A second part in the development of a generic flow injection analysis (FIA) method to determine compounds with a Secondary Amine or amide in their structure is described. This part consists in the selection and evaluation of the chemical reaction conditions. Sodium hypochlorite first converts the Secondary Amine or the amide to a primary Amine. The latter reacts with o-phthalaldehyde (OPA) and a thiol (N-acetylcysteine (NAC)) to form a derivative which can be measured fluorimetrically. To investigate the influence of the different chemical reaction parameters on the peak height for a set of 31 pharmaceutical compounds, a quarter-fraction factorial design for six factors at two levels (26–2-resolution IV, 16 experiments) was executed. Effects on the responses were calculated for each compound. Parallel coordinate geometry (PCG) plots and principal component analysis (PCA) were also applied on the measured responses as aids in the interpretation of the results.
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development of a generic flow injection analysis method for compounds with a Secondary Amine or amide function using an experimental design approach i selection and evaluation of the fia system parameters
Analytica Chimica Acta, 2001Co-Authors: C Vannecke, M S Bloomfield, Vander Y Heyden, E Van Gyseghem, T J Coomber, D L MassartAbstract:Abstract A generic flow injection analysis (FIA) method to determine compounds with a Secondary Amine or an amide in their structure was developed. A first part of the development, namely the selection and evaluation of the FIA system, is described. A chemical reaction with sodium hypochlorite (NaOCl) first converts the Secondary Amine or the amide to a primary Amine. This is followed by reaction of the primary Amine with o-phthalaldehyde (OPA) and a thiol (N-acetylcysteine, NAC), to form a derivative which can be measured fluorimetrically. To investigate the influence of the different FIA system parameters on both the peak height and the residence time for a set of 28 pharmaceutical compounds, a half-fraction factorial design for five factors at two levels (25−1: resolution V=16 experiments) was executed. Effects on both responses were calculated. Since the peak height should be maximized and the residence time minimized, the Pareto optimality concept was applied to make an optimal compromise between both responses and to eventually select a generic FIA system.
