| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 10591283 | Bioorganic & Medicinal Chemistry Letters | 2013 | 6 Pages |
Abstract
A series of new 4â³-O-desosaminyl clarithromycin derivatives were designed and synthesized. The efficient synthesis routes of 6-deoxy-desosamine donors 8 and 11 were developed and the methodology of glycosylation of clarithromycin 4â³-OH with desosamine was studied. The activities of the target compounds were tested against a series of macrolide-sensitive and macrolide-resistant pathogens. Some of them showed activities against macrolide sensitive pathogens, and compounds 19 and 22 displayed significant improvement of activities against sensitive pathogens and two strains of MRSE, which verified the importance of desosamine in the interaction of macrolide and its receptor, and offered valuable information of the SAR of macrolide 4â³-OH derivatives.
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Authors
Di Zhu, Yanpeng Xu, Yi Liu, Xiaozhuo Chen, Zhehui Zhao, Pingsheng Lei,