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Bioorg Med Chem Lett. 2013 Sep 15;23(18):5057-60. doi: 10.1016/j.bmcl.2013.07.042. Epub 2013 Jul 25.

Design, synthesis and biological evaluation of azithromycin glycosyl derivatives as potential antibacterial agents.

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  • 1Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China.


A series of 11,12-cyclic carbonate azithromycin-4″-O-carbamoyl glycosyl derivatives were designed, synthesized, and evaluated as antibacterial agents to search for target compounds with excellent activity. The results of preliminary antibacterial tests against eight strains in vitro revealed that all of the title compounds exhibited improved activities with broad spectrum compared with the parent compound. The glycosylated side chains may be the pharmacophores responsible for the improved activity.

Copyright © 2013 Elsevier Ltd. All rights reserved.


Antibacterial activity; Azithromycin; Glycosyl; Synthesis

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