Synthesis and antibacterial activity of 4- and 8-methoxy trinems

被引:25
作者
Andreotti, D
Rossi, T
Gaviraghi, G
Donati, D
Marchioro, C
DiModugno, E
Perboni, A
机构
[1] Glaxo Research Laboratories, 37138 Verona
关键词
D O I
10.1016/0960-894X(96)00056-X
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The synthesis of all the isomers of 8-methoxy-(9S,10S,12R)-10-(1-hydroxyethyl)-11-oxo-1-azatricyclo-[7.2.0.0(3,8])-undec-2-ene-carboxylates 2 and 4-methoxy-(9R,10S,12R)-10-(1-hydroxyethyl)-11-oxo-1-azatricyclo-[7.2.0.0(3.8)]-undec-2-ene-carboxylates 3 is described. The biological data obtained indicated that the (4S,8S)-4-methoxy derivative (3b) is the best compound in terms of microbiological activity, breadth of spectrum of action and stability to hydrolytic enzymes, namely beta-lactamases.
引用
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页码:491 / 496
页数:6
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