Synthesis and antibacterial activity of novel modified 5-O-desosamine ketolides.

Xiaozhuo Chen, Peng Xu, Yanpeng Xu, Lu Liu, Yi Liu, Di Zhu, Pingsheng Lei

State Key Laboratory of Bioactive Substances and Functions of Natural Medicines, Beijing Key Laboratory of Active Substances Discovery and Drugability Evaluation, Department of Medicinal Chemistry, Institute of Materia Medica, Peking Union Medical College, Chinese Academy of Medical Sciences, Beijing 100050, PR China.

Bioorganic & medicinal chemistry letters 2012 Dec 15

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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.

Citation

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