Synthesis and antibacterial activity of 4″-O-carbamoyl analogs of clarithromycin  

作　　者：Xue Cui Shen Bo Jiao Shu Tao Ma 

机构地区：[1]School of Pharmaceutical Sciences,Shandong University,Jinan 250012,China

出　　处：《Chinese Chemical Letters》2010年第3期257-260,共4页中国化学快报（英文版）

基　　金：supported by Major R&D Program of New Drugs-National S&T Key Special Subject of China (No.2009ZX09103-115);National Natural Science Foundation of China(No.20872081);Natural Science Foundation of Shandong(No.Y2006C31)

摘　　要：A series of novel 4'-O-carbamoyl analogs of clarithromycin were synthesized and evaluated for their in vitro antibacterial activity. All of the desired compounds showed excellent activity against erythromycin-susceptible S.pneumoniae.Particularly,4-fluorobenzyl carbamate 7a demonstrated potent activity against erythromycin-resistant S.pneumoniae encoded by the mef gene,and remarkably improved activity against erythromycin-resistant S.pneumoniae encoded by the erm gene,and the erm and mef genes.A series of novel 4'-O-carbamoyl analogs of clarithromycin were synthesized and evaluated for their in vitro antibacterial activity. All of the desired compounds showed excellent activity against erythromycin-susceptible S.pneumoniae.Particularly,4-fluorobenzyl carbamate 7a demonstrated potent activity against erythromycin-resistant S.pneumoniae encoded by the mef gene,and remarkably improved activity against erythromycin-resistant S.pneumoniae encoded by the erm gene,and the erm and mef genes.

关 键 词：Clarithromycin analogs 4″-O-carbamate SYNTHESIS Antibacterial activity Resistant bacteria 

分 类 号：R914[医药卫生—药物化学]