New class of methyl tetrazole based hybrid of (Z)-5-benzylidene-2-(piperazin-1-yl)thiazol-4(%H)-one as potent antitubercular agents

被引：38

作者：

Chauhan, Kuldeep ^{[1
]}

Sharma, Moni ^{[1
]}

Trivedi, Priyanka ^{[2
]}

Chaturvedi, Vinita ^{[2
]}

Chauhan, Prem M. S. ^{[1
]}

机构：

[1] CSIR, Cent Drug Res Inst, Med & Proc Chem Div, Lucknow 226031, Uttar Pradesh, India

[2] CSIR, Cent Drug Res Inst, Drug Target Discovery & Dev Div, Lucknow 226031, Uttar Pradesh, India

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2014年 / 24卷 / 17期

关键词：

Rhodanine; Tetrazole; Mycobacterium tuberculosis; Cytotoxicity; MYCOBACTERIUM-TUBERCULOSIS; RHODANINE; DERIVATIVES; DISCOVERY; INHIBITORS; SCAFFOLDS; TARGET;

D O I：

10.1016/j.bmcl.2014.07.061

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

In search of potential therapeutics for tuberculosis, we describe here the synthesis and in vitro antitubercular activity of a novel series of thiazolone piperazine tetrazole derivatives. Among all the synthesized derivatives, four compounds (10, 14,20 and 33) exhibited more potent activity (MIC = 3.08, 3.01, 2.62 and 2.51 mu M) than ethambutol (MIC = 9.78 mu M) and pyrazinamide (MIC = 101.53 mu M) against Mycobacterium tuberculosis. Furthermore, they displayed no toxicity against Vero cells (C1008) and mouse bone marrow derived macrophages (MBMDM phi)). These investigated analogues have emerged as possible lead molecule to enlarge the scope of the study. (C) 2014 Published by Elsevier Ltd.

引用

页码：4166 / 4170

页数：5

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