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