Synthesis and antibacterial activity of novel modified 5-O-desosamine ketolides
2012
Chen, Xiaozhuo | Xu, Peng | Xu, Yanpeng | Liu, Lu | Liu, Yi | Zhu, Di | Lei, Pingsheng
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.
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