Antimycobacterial Evaluation of Pyrazinoic Acid Reversible Derivatives

被引：18

作者：

Dolezal, Martin ^{[1
]}

Kesetovic, Diana ^{[1
]}

Zitko, Jan ^{[1
]}

机构：

[1] Charles Univ Prague, Fac Pharm Hradec Kralove, Dept Pharmaceut Chem & Pharmaceut Anal, Hradec Kralove 50005, Czech Republic

来源：

CURRENT PHARMACEUTICAL DESIGN | 2011年 / 17卷 / 32期

关键词：

Pyrazines; in vitro antimycobacterial evaluation; structure-activity relationships; SUBSTITUTED N-PHENYLPYRAZINE-2-CARBOXAMIDES; MYCOBACTERIUM-TUBERCULOSIS; DRUG-RESISTANT; PYRAZINAMIDE; ANTIFUNGAL;

D O I：

10.2174/138161211798194477

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Design, results of in vitro antimycobacterial evaluation, and study of structure-activity relationships of various pyrazinecarboxylic acid reversible derivatives are presented. This review deals with some pyrazinamide analogues/prodrugs derived from N-phenylpyrazine-2-carboxamides (1), arylaminopyrazine-2,5-dicarbonitriles (2), aryl/alkylsulphanylpyrazines (3,4), and aroylpyrazines (5) effecting >50% inhibition in the primary antimycobacterial screen. The promising pyrazine candidates for further antimycobacterial evaluation were discovered. Results give good view onto structure-activity relationships of these analogues and promise even better activity of new compounds prepared after some structure optimization experiments.

引用

页码：3506 / 3514

页数：9

共 42 条

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