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A series of novel modified 5-O-desosamine-ketolides were synthesized. The 5-O-desosamine fragment was removed from ketolide by an efficient and mild manipulation. 4-O-substituted desosamine was introduced into the ketolide aglycon and various coupling methods were essayed for the glycosylation. Three novel ketolides were tested for in vitro antibacterial activity against a panel of susceptible and resistant pathogens. Compound 26 showed potent activity against all the methicillin-sensitivity and resistant pathogens. Copyright © 2012 Elsevier Ltd. All rights reserved.


Xiaozhuo Chen, Peng Xu, Yanpeng Xu, Lu Liu, Yi Liu, Di Zhu, Pingsheng Lei. Synthesis and antibacterial activity of novel modified 5-O-desosamine ketolides. Bioorganic & medicinal chemistry letters. 2012 Dec 15;22(24):7402-5

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PMID: 23122862

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