4.7 Article

Synthesis and evaluation of anti-tubercular and antibacterial activities of new 4-(2,6-dichlorobenzyloxy)phenyl thiazole, oxazole and imidazole derivatives. Part 2

期刊

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 49, 期 -, 页码 164-171

出版社

ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2012.01.007

关键词

4-(2,6-dichlorobenzyloxy)phenyl thiazole derivatives; Anti-tubercular activity; Antibacterial activity

资金

  1. Significant new drugs development Science and Technology Major Projects of China [2009ZX09501-003]
  2. Innovation Program for the Postgraduates in China Pharmaceutical University, P.R.China

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A series of substituted 4-(2,6-dichlorobenzyloxy)phenyl thiazole, oxazole and imidazole derivatives were synthesized. The derivatives were screened for in vitro anti-tubercular activities against Mycobacterium tuberculosis H37Rv using the Microplate Alamar Blue Assay (MABA), and antibacterial activities with agar dilution method against clinical S. aureus, E. coli, S. pneumoniae and penicilin-resistant S. pneumoniae. Among 15 compounds, several thiazole derivatives exhibited good anti-tubercular activities with MIC values between 1 mu M and 61.2 mu M, and potent activities against S. pneumoniae with MIC values less than 0.134 mu M. These studies suggest that the thiazole scaffold may serve as a new promising template for further elaboration as anti-tubercular and antibacterial drugs. (C) 2012 Elsevier Masson SAS. All rights reserved.

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