Synthesis and antibacterial activity of a series of novel 9-O-acetyl- 4'-substituted 16-membered macrolides derived from josamycin.

作者: Zhehui Zhao , Longlong Jin , Yanpeng Xu , Di Zhu , Yi Liu

DOI: 10.1016/J.BMCL.2013.12.029

关键词: MicrobiologyChemistryJosamycinStereochemistryStaphylococcus epidermidisAntibacterial activityIn vitroStaphylococcus aureus

摘要: Abstract A series of novel 9-O-acetyl-4′-substituted 16-membered macrolides derived from josamycin has been designed and synthesized by cleavage the mycarose subsequent modification 4′-hydroxyl group. These derivatives were evaluated for their in vitro antibacterial activities against a panel Staphylococcus aureus epidermidis. 15 (4′-O-(3-Phenylpropanoyl)-9-O-acetyl-desmycarosyl josamycin) 16 (4′-O-butanoyl-9-O-acetyl-desmycarosyl exhibited comparable to S. (MSSA) epidermidis (MSSE).

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