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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.

Abstract
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 (MBMDMϕ). These investigated analogues have emerged as possible lead molecule to enlarge the scope of the study.
AuthorsKuldeep Chauhan, Moni Sharma, Priyanka Trivedi, Vinita Chaturvedi, Prem M S Chauhan
JournalBioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 24 Issue 17 Pg. 4166-70 (Sep 01 2014) ISSN: 1464-3405 [Electronic] England
PMID25127167 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
CopyrightCopyright © 2014. Published by Elsevier Ltd.
Chemical References
  • Antitubercular Agents
  • Tetrazoles
  • Thiazoles
Topics
  • Animals
  • Antitubercular Agents (chemical synthesis, chemistry, classification, pharmacology)
  • Chlorocebus aethiops
  • Dose-Response Relationship, Drug
  • Microbial Sensitivity Tests
  • Molecular Structure
  • Mycobacterium tuberculosis (drug effects)
  • Structure-Activity Relationship
  • Tetrazoles (chemical synthesis, chemistry, pharmacology)
  • Thiazoles (chemical synthesis, chemistry, pharmacology)
  • Vero Cells

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