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

  作者 Lu, XY; Liu, XB; Wan, BJ; Franzblau, SG; Chen, LL; Zhou, CL; You, QD  
  选自 期刊  European Journal of Medicinal Chemistry;  卷期  2012年49-1;  页码  164-171  
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[摘要]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. coil, 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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