期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 22, 期 15, 页码 4942-4945出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.06.039
关键词
Synthesis; Clostridium difficile; Antibacterial activity; Demethylvancomycin; Analogue
资金
- National Natural Science Foundation of China [81172920]
- National Science and Technology Major Project of China [2009ZXJ09004-090, 2012ZX09J12108-05C]
- National Basic Research Program of China (973 Program) [2010CB912603]
To explore the structure-activity relationships (SAR) of demethylvancomycin (2) and find more effective new chemical entities than known glycopeptides for the treatment of Clostridium difficile (C. difficile), 17 novel N-substituted (N-arylmethylene or -aliphatic substituents) demethylvancomycin derivatives were prepared. These analogues have been evaluated in vitro for their antibacterial activities against C. difficile and Enterococcus faecium (E. faecium). Compounds 5d, 5h, and 5i with N-arylmethylene substituents, structurally similar to Oritavancin, showed more potent antibacterial activity against C. difficile than vancomycin (1) or demethylvancomycin (2). Meanwhile, compound 5k with an undecyl side chain showed the most potent antibacterial activity against E. faecium (vancomycin-resistant strain). Crown Copyright (c) 2012 Published by Elsevier Ltd. All rights reserved.
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