陈佩林, 杨祯祥, 彭司勋. N-(2-巯基苯甲酰)-N-烷基/芳基甘氨酸及其双硫化物的合成J. 药学学报, 1987, 22(9): 662-670.
引用本文: 陈佩林, 杨祯祥, 彭司勋. N-(2-巯基苯甲酰)-N-烷基/芳基甘氨酸及其双硫化物的合成J. 药学学报, 1987, 22(9): 662-670.
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CHEN Pei-Lin, YANG Zhen-Xiang , PENG Si-Xun, . SYNTHESIS OF N-(2-MERCAPTOBENZOYL)-N-(ALKYL/ARYL)-GLYCINES AND THE CORRESPONDING DISULFIDESJ. Acta Pharmaceutica Sinica, 1987, 22(9): 662-670.
Citation: CHEN Pei-Lin, YANG Zhen-Xiang , PENG Si-Xun, . SYNTHESIS OF N-(2-MERCAPTOBENZOYL)-N-(ALKYL/ARYL)-GLYCINES AND THE CORRESPONDING DISULFIDESJ. Acta Pharmaceutica Sinica, 1987, 22(9): 662-670.
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N-(2-巯基苯甲酰)-N-烷基/芳基甘氨酸及其双硫化物的合成

SYNTHESIS OF N-(2-MERCAPTOBENZOYL)-N-(ALKYL/ARYL)-GLYCINES AND THE CORRESPONDING DISULFIDES

    摘要
  • 摘要: 为了寻找新的血管紧张素转化酶抑制剂(ACEI),本文根据血管紧张素转化酶(ACE)活性部位及与底物或抑制剂的作用模式,以及现有ACEI的结构特征,设计合成了16个N-(2-巯基苯甲酰)-N-烷基/芳基甘氨酸(Ⅰ1～8)及其双硫化物(Ⅱ1～8)。其中,化合物Ⅰ3,Ⅱ1降压活性(大鼠)最强,与巯甲丙腑酸(captopril)相似。

     

    Abstract: In order to search for new angiotensin-converting enzyme inhibitors (ACEI), a series of N-(2-mercaptobenzoyl)-N-(alkyl/aryl)-glycines (I1～8) and the corresponding disulfides (Ⅱ1～8 were synthesized.Compounds I1～8 were prepared by the condensation of 2,2'-dithiobisbenzoyl dichloride with ethyl N-alkyl/aryl glycinate, followed by reduction and hydrolysis.Compounds Ⅱ1～8 were obtained by the oxidation of compounds I1～8 with hydrogen peroxide (30%) in weak alkali medium below 10℃In preliminary test in rats, compounds I3 and Ⅱ1 showed marked hypotensive activity.

     

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