THE SYNTHESIS AND LACTAMASE INHIBITORY ACTIVITY OF 6-(CARBOXYMETHYLENE)PENICILLINS AND 7-(CARBOXYMETHYLENE)CEPHALOSPORINS

被引：23

作者：

BUYNAK, JD

GENG, B

BACHMANN, B

HUA, L

机构：

[1] Department of Chemistry, Southern Methodist University, Dallas

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1995年 / 5卷 / 14期

关键词：

D O I：

10.1016/0960-894X(95)00249-S

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 6-(carboxymethylene)penicillinates and 7-(carboxymethylene)cephalosporanates were synthesized and evaluated as inhibitors of one type A and two type C beta-lactamases. Disodium 6-(carboxymethylene)penicillinate sulfone (15) showed broad spectrum activity. A kinetic analysis demonstrated that 15 was a potent, partially irreversible inhibitor of the beta-lactamase derived from Enterobacter cloacae P99.

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页码：1513 / 1518

页数：6

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