Novel C-2 Substituted Carbapenem Derivatives Part I. Synthesis and Biological Activity of Non-aromatic Heterocyclic Derivatives

GEORGE BURTON; NICOLA J. C. CLEAR; A. JOHN EGLINGTON; ANGELA W. GUEST; ERIC HUNT; ANTOINETTE NAYLOR; MICHAEL J. PEARSON; ANDREW K. TAKLE

doi:10.7164/antibiotics.49.1258

Novel C-2 Substituted Carbapenem Derivatives

Part I. Synthesis and Biological Activity of Non-aromatic Heterocyclic Derivatives

GEORGE BURTON, NICOLA J. C. CLEAR, A. JOHN EGLINGTON, ANGELA W. GUEST, ERIC HUNT, ANTOINETTE NAYLOR, MICHAEL J. PEARSON, ANDREW K. TAKLE

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JOURNAL FREE ACCESS

1996 Volume 49 Issue 12 Pages 1258-1265

DOI https://doi.org/10.7164/antibiotics.49.1258

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Abstract

A new series of carbapenems, having a saturated or partially unsaturated heterocycle at C-2, has been synthesised. The in vitro antibacterial activity of these compounds and their stability to human dehydropeptidase-1 (DHP-1) are described. The stereochemistry of the C-2 side-chain and the presence of a double bond in the heterocycle were shown to have significant effects on the stabilities of the compounds to DHP-1.

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