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Synthesis and biological evaluation of a novel series of 1,5-benzothiazepine derivatives as potential antimicrobial agents

  作者 Wang, LZ; Zhang, P; Zhang, XM; Zhang, YH; Li, Y; Wang, YX  
  选自 期刊  European Journal of Medicinal Chemistry;  卷期  2009年44-7;  页码  2815-2821  
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[摘要]Two series of novel 1,5-benzothiazepine derivatives (23 compounds) were efficiently synthesized and evaluated for antibacterial and antifungal activities. The results indicated that the compounds possessed a broad spectrum of activity against the tested microorganisms and showed higher activity against fungi than bacteria. Compound 2e exhibited the greatest antimicrobial activity. Preliminary study of the structure-activity relationship revealed that substituents in phenyl rings had a great effect on the antimicrobial activity of these compounds. (C) 2008 Published by Elsevier Masson SAS.

 
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