Novel 3-deoxy-3-descladinosyl-6-O-methyl erythromycin A analogues. Synthesis and in vitro activity.

被引:27
作者
Elliott, RL
Pireh, D
Nilius, AM
Johnson, PM
Flamm, RK
Chu, DTW
Plattner, JJ
Or, YS
机构
[1] Anti-Infective Discovery Research, Pharmaceutical Prod. Res. Division, Abbott Laboratories, Abbott Park, IL 60064-3500
[2] Dept. 47N, Abbott Park, IL 60064-3500
关键词
D O I
10.1016/S0960-894X(97)00078-4
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of novel 3-deoxy-3-des-cladinosyl-6-O-methyl erythromycin A analogues has been synthesized and evaluated in vitro for antibacterial activity. These analogues were readily synthesized by tributyltin hydride-mediated radical reduction of a 3-O-xanthyl intermediate to afford the 3-deoxy macrolide. A number of oxime, carbonate, and carbamate derivatives were synthesized and evaluated for antibacterial activity. Overall, these analogues had fairly good antibacterial activity against gram-positive bacteria, although they were generally less potent than the corresponding 3-O-cladinosyl or 3-keto analogues. (C) 1997 Elsevier Science Ltd. All rights reserved.
引用
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页码:641 / 646
页数:6
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