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J Antibiot (Tokyo). 1997 Mar;50(3):237-45.

Novel C-2 substituted carbapenem derivatives. Part III. Synthesis and biological activity of 2-(functionalised ethenyl, oxyiminomethyl and alpha-.

The Journal of antibiotics

Clear, Davies, Eglington, Fell, Hinks, Hird, Hunt, Moss, Pearson

Affiliations

  1. SmithKline Beecham Pharmaceuticals, Betchworth, Surrey, U.K.

PMID: 9439695

Abstract

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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