Novel C-2 substituted carbapenem derivatives. Part III. Synthesis and biological activity of 2-(functionalised ethenyl, oxyiminomethyl and alpha-
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.
Clear
NJ
SmithKline Beecham Pharmaceuticals, Betchworth, Surrey, U.K.
Davies
JS
Eglington
AJ
Fell
SC
Hinks
JD
Hird
NW
Hunt
E
Moss
SF
Pearson
MJ