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

IR@CDRI: CSIR-Central Drug Research Institute, Lucknow

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Field Value
 
Creator Chauhan, Kuldeep
Sharma, Moni
Trivedi, Priyanka
Chaturvedi, Vinita
Chauhan, P. M. S.
 
Date 2014-10-27T11:13:11Z
2014-10-27T11:13:11Z
2014
 
Identifier Bioorganic & Medicinal Chemistry Letters, 2014, 24 (17), 4166–4170
http://hdl.handle.net/123456789/1419
 
Description 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 μM) than ethambutol (MIC = 9.78 μM) and pyrazinamide (MIC = 101.53 μM) against Mycobacterium tuberculosis. Furthermore, they displayed no toxicity against Vero cells (C1008) and mouse bone marrow derived macrophages (MBMDMɸ). These investigated analogues have emerged as possible lead molecule to enlarge the scope of the study.
 
Format 267035 bytes
application/pdf
 
Language en
 
Relation CSIR-CDRI Communication No. 8738
 
Subject Rhodanine
Tetrazole
Mycobacterium tuberculosis
Cytotoxicity
 
Title New class of methyl tetrazole based hybrid of (Z)-5-benzylidene-2-(piperazin-1-yl) thiazol-4(%H)-one as potent antitubercular agents
 
Type Article