title: Novel C-2 substituted carbapenem derivatives. Part I. Synthesis and biological activity of non-aromatic heterocyclic derivatives.
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.
authors.affiliation: SmithKline Beecham Pharmaceuticals, Brockham Park, Betchworth, Surrey, U.K.
authors.forename: G
authors.initials: G
authors.lastname: Burton
authors.forename: N J
authors.initials: NJ
authors.lastname: Clear
authors.forename: A J
authors.initials: AJ
authors.lastname: Eglington
authors.forename: A W
authors.initials: AW
authors.lastname: Guest
authors.forename: E
authors.initials: E
authors.lastname: Hunt
authors.forename: A
authors.initials: A
authors.lastname: Naylor
authors.forename: M J
authors.initials: MJ
authors.lastname: Pearson
authors.forename: A K
authors.initials: AK
authors.lastname: Takle
mesh_terms: D001419:Bacteria / Q000187:drug effects*; D015780:Carbapenems / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D004150:Dipeptidases / Q000378:metabolism; D006801:Humans; D008826:Microbial Sensitivity Tests; D008968:Molecular Conformation; D015394:Molecular Structure
chemical_list: D015780:Carbapenems; D004150:Dipeptidases; C038937:dipeptidase