SYNTHESIS AND BIOLOGICAL-ACTIVITY OF NOVEL CEPHALOSPORINS CONTAINING A (Z)-VINYL DIMETHYLPHOSPHONATE GROUP

被引：28

作者：

SMITH, PW ^{[1
]}

CHAMIEC, AJ ^{[1
]}

CHUNG, G ^{[1
]}

COBLEY, KN ^{[1
]}

DUNCAN, K ^{[1
]}

HOWES, PD ^{[1
]}

WHITTINGTON, AR ^{[1
]}

WOOD, MR ^{[1
]}

机构：

[1] GLAXO GRP RES LTD,RES & DEV,DEPT CHEMOTHERAPY,GREENFORD UB6 0HE,MIDDX,ENGLAND

来源：

JOURNAL OF ANTIBIOTICS | 1995年 / 48卷 / 01期

关键词：

D O I：

10.7164/antibiotics.48.73

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：

A series of cephalosporins containing a novel 7-[2-(Z)-(2-amino-thiazol-4-yl)-3-(dimethoxyphosphoryl)-acryloylamino] group were prepared and their antibacterial activity measured against a range of pathogens. In general the compounds displayed a broad spectrum of activity against both Gram positive and Gram negative organisms, except Pseudomonas aeruginosa. Activity against the latter could be achieved by introducing a catechol moiety at the 3 position of the cephalosporin. The methyl phosphonates in general were stable to a wide range of beta-lactamases, including the TEM enzymes and the Enterobacter cloacae P99 chromosomal enzyme. In addition, they showed the advantage of being highly water soluble.

引用

页码：73 / 82

页数：10

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