BETA-LACTAMASE-STABLE PENICILLINS - SYNTHESIS AND STRUCTURE-ACTIVITY-RELATIONSHIPS OF (Z)-ALKYLOXYIMINO PENICILLINS - SELECTION OF BRL 44154

被引：14

作者：

BROWN, P ^{[1
]}

CALVERT, SH ^{[1
]}

CHAPMAN, PCA ^{[1
]}

COSHAM, SC ^{[1
]}

EGLINGTON, AJ ^{[1
]}

ELLIOT, RL ^{[1
]}

HARRIS, MA ^{[1
]}

HINKS, JD ^{[1
]}

LOWTHER, J ^{[1
]}

MERRIKIN, DJ ^{[1
]}

PEARSON, MJ ^{[1
]}

PONSFORD, RJ ^{[1
]}

SYMS, JV ^{[1
]}

机构：

[1] SMITHKLINE BEECHAM PHARMACEUT,DIV RES,BROCKHAM PK,BETCHWORTH RH3 7AJ,SURREY,ENGLAND

来源：

JOURNAL OF THE CHEMICAL SOCIETY-PERKIN TRANSACTIONS 1 | 1991年 / 04期

关键词：

D O I：

10.1039/p19910000881

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A series of (Z)-2-alkyloxyimino-2-(2-aminothiazol-4-yl)acetamidopenicillins has been prepared. New methodology has been developed to prepare tertiary alkyl oximes. High stability to beta-lactamases and potent antibacterial activity have been achieved against Gram-positive and certain Gram-negative organisms. Activity against methicillin-resistant Staphylococcus aureus was an unexpected finding. The cyclopentyl analogue 4f, BRL 44154, has been selected for further study.

引用

页码：881 / 891

页数：11

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