期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 24, 期 17, 页码 4166-4170出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2014.07.061
关键词
Rhodanine; Tetrazole; Mycobacterium tuberculosis; Cytotoxicity
资金
- Council of Scientific and Industrial Research (CSIR, India)
- Indian Council of Medical Research (ICMR, India)
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.
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