Ring-substituted imidazoles as a new class of anti-tuberculosis agents

被引：90

作者：

Gupta, P ^{[1
]}

Hameed, S ^{[1
]}

Jain, R ^{[1
]}

机构：

[1] Natl Inst Pharmaceut Educ & Res, Dept Med Chem, SAS Nagar 160062, Punjab, India

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2004年 / 39卷 / 09期

关键词：

tuberculosis; homolytic free radical reaction; ring-substituted-1H-imidazole-4-carboxylic acid derivatives; 3-(2-alkyl-1H-imidazol-4-yl)-propionic; acid derivatives;

D O I：

10.1016/j.ejmech.2004.05.005

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We describe in vitro anti-Mycobacterium tuberculosis activities of ring-substituted- 1H-imidazole-4-carboxylic acid derivatives (1-6), and 3-(2-alkyl-1H-imidazol-4-yl)-propionic acid derivatives (7-13) against drug-sensitive and drug-resistant M. tuberculosis H37Rv strains. The most effective analogues, 2f (R=R1=c-C5H9), and 2h (R=R-1 =c-C6H11) have produced >90% inhibition at a concentration of <6.25 mug/ml in the drug-sensitive screen. Upon further evaluation against drug-resistant strains, both analogues 2f and 2h produced an MIC value of 25.0 mug/ml. The observation of significant anti -tuberculosis activity in some of these analogues describes the discovery of novel ring-substituted-1H-imidazole-4-carboxylic acid ethyl esters as a new class of anti-tuberculosis agents. (C) 2004 Elsevier SAS. All rights reserved.

引用

页码：805 / 814

页数：10

共 16 条

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