Novel C-2 substituted carbapenem derivatives .3. Synthesis and biological activity of 2-(functionalised ethenyl, oxyimino methyl and alpha-[hydroxy]benzyl)-carbapenems

被引:2
作者
Clear, NJC [1 ]
Davies, JS [1 ]
Eglington, AJ [1 ]
Fell, SCM [1 ]
Hinks, JD [1 ]
Hird, NW [1 ]
Hunt, E [1 ]
Moss, SF [1 ]
Pearson, MJ [1 ]
机构
[1] SMITHKLINE BEECHAM PHARMACEUT,BETCHWORTH RH3 7AJ,SURREY,ENGLAND
关键词
D O I
10.7164/antibiotics.50.237
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
The synthesis, antibacterial activity and stability to human dehydropeptidase-1 (DHP-1) of three small series of carbapenems carrying carbon-linked substituents at C-2 are described. C-2 Ethenyl carbapenems showed moderate antibacterial activity but poor stability to DHP-1. C-2 Oxyiminomethyl carbapenems demonstrated variable activity and stability. C-2 alpha-(Hydroxy)benzyl carbapenems were the most promising and showed good potency and DHP-1 stability.
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页码:237 / 245
页数:9
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