6-(SUBSTITUTED METHYLENE)PENEMS, POTENT BROAD-SPECTRUM INHIBITORS OF BACTERIAL BETA-LACTAMASE .3. STRUCTURE-ACTIVITY-RELATIONSHIPS OF THE 5-MEMBERED HETEROCYCLIC-DERIVATIVES

被引：40

作者：

BENNETT, I

BROOM, NJP

BRUTON, G

CALVERT, S

CLARKE, BP

COLEMAN, K

EDMONDSON, R

EDWARDS, P

JONES, D

OSBORNE, NF

WALKER, G

机构：

[1] SmithKline Beecham Pharmaceuticals, Chemotherapeutic Research Centre, Brockham Park, Betchworth, Surrey

来源：

JOURNAL OF ANTIBIOTICS | 1991年 / 44卷 / 03期

关键词：

D O I：

10.7164/antibiotics.44.331

中图分类号：

Q81 [生物工程学（生物技术）]; Q93 [微生物学];

学科分类号：

071005 ; 0836 ; 090102 ; 100705 ;

摘要：

Sodium (5RS)-Z-6-(heterocyclylmethylene)penem-3-carboxylates (2) are a series of extremely potent inhibitors of bacterial beta-lactamases. A variety of 5-membered heteroaromatic derivatives have been prepared and structure-activity studies reveal a preferred substituent orientation. One of these derivatives, the 1-methyl-1,2,3-triazolyl compound (5m) is a more potent synergist of amoxycillin than clavulanic acid, sulbactam or tazobactam.

引用

页码：331 / 337

页数：7

共 6 条

[1] 6-(SUBSTITUTED METHYLENE)PENEMS, POTENT BROAD-SPECTRUM INHIBITORS OF BACTERIAL BETA-LACTAMASE .1. RACEMIC 6-ETHYLIDENEPENEMS [J].