title: Structure-activity relationships of biphenyl tetrazoles as metallo-beta-lactamase inhibitors.
abstract: Resistance to carbapenem antibiotics in gram-negative bacteria is due, in part, to expression of a wide spectrum metallo-beta-lactamase, which renders the drug inactive. Biphenyl tetrazoles containing 3-n-butyl-1-phenylpyrazole-5-carboxylates or the corresponding 5-ethyl esters were found to inhibit metallo-beta-lactamases as well as renal dehydropeptidase I to a lesser extent.
authors.affiliation: Department of Biochemistry, Merck Research Laboratories, Rahway, NJ 07065-0900, USA.
authors.forename: J H
authors.initials: JH
authors.lastname: Toney
authors.forename: K A
authors.initials: KA
authors.lastname: Cleary
authors.forename: G G
authors.initials: GG
authors.lastname: Hammond
authors.forename: X
authors.initials: X
authors.lastname: Yuan
authors.forename: W J
authors.initials: WJ
authors.lastname: May
authors.forename: S M
authors.initials: SM
authors.lastname: Hutchins
authors.forename: W T
authors.initials: WT
authors.lastname: Ashton
authors.forename: D E
authors.initials: DE
authors.lastname: Vanderwall
mesh_terms: D001441:Bacteroides fragilis / Q000201:enzymology; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013777:Tetrazoles / Q000737:chemistry* / Q000494:pharmacology*; D065093:beta-Lactamase Inhibitors
chemical_list: D004791:Enzyme Inhibitors; D013777:Tetrazoles; D065093:beta-Lactamase Inhibitors