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Novel C-2 substituted carbapenem derivatives. Part I. Synthesis and biological activity of non-aromatic heterocyclic derivatives. 1996
G Burton, and
N J Clear, and
A J Eglington, and
A W Guest, and
E Hunt, and
A Naylor, and
M J Pearson, and
A K Takle
SmithKline Beecham Pharmaceuticals, Brockham Park, Betchworth, Surrey, U.K.
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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