Novel imidazo[2,1-b][1,3,4]thiadiazole carrying rhodanine-3-acetic acid as potential antitubercular agents

被引：134

作者：

Alegaon, Shankar G. ^{[1
]}

Alagawadi, Kallanagouda R. ^{[1
]}

Sonkusare, Pranali V. ^{[1
]}

Chaudhary, Sagar M. ^{[1
]}

Dadwe, Dilip H. ^{[1
]}

Shah, Amol S. ^{[1
]}

机构：

[1] KLE Univ Coll Pharm, Dept Pharmaceut Chem, Belgaum 590010, Karnataka, India

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2012年 / 22卷 / 05期

关键词：

Imidazo[2,1-b][1,3,4]thiadiazole; Thiazolidine-2,4-diones; Rhodanine acetic acid; Drug-likeness; Antitubercular activity; INHIBITION; RHODANINES; SAR;

D O I：

10.1016/j.bmcl.2012.01.052

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The increase in the prevalence of multi drug-resistant and extensively drug-resistant strains of Mycobacterium tuberculosis case demonstrates the urgent need of discovering new promising compounds with antimycobacterial activity. As part of our research program and with a aim of identifying new antitubercular drug candidates, a new class of 2-(trifluoromethyl)-6-arylimidazo[2,1-b][1,3,4] thiadiazole derivatives has been synthesized by both conventional as well as microwave assisted method and evaluated for their in vitro antitubercular activity against M. tuberculosis H(37)Rv. Moreover, various drug-likeness properties of new compounds were predicted. Seven compounds from the series exhibited good activity with MIC in range 3.12-1.56 mu g/ml. The present study suggests that compounds 6b, 6c, 6d, 6e and 6f may serve as promising lead scaffolds for further generation of new anti-TB agents. (c) 2012 Elsevier Ltd. All rights reserved.

引用

页码：1917 / 1921

页数：5

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