title: Inhibitors of the FEZ-1 metallo-beta-lactamase.
abstract: Metallo-beta-lactamases (MBLs) catalyze the hydrolysis of beta-lactams including penicillins, cephalosporins and carbapenems. Starting from benzohydroxamic acid (1) structure-activity studies led to the identification of selective inhibitors of the FEZ-1 MBL, e.g., 2,5-substituted benzophenone hydroxamic acid 17 has a K(i) of 6.1+/-0.7microM against the FEZ-1 MBL but does not significantly inhibit the IMP-1, BcII, CphA or L1 MBLs.
authors.affiliation: Chemistry Research Laboratory, 12 Mansfield Road, Oxford, United Kingdom.
authors.forename: Benoît M R
authors.initials: BM
authors.lastname: Liénard
authors.forename: Louise E
authors.initials: LE
authors.lastname: Horsfall
authors.forename: Moreno
authors.initials: M
authors.lastname: Galleni
authors.forename: Jean-Marie
authors.initials: JM
authors.lastname: Frère
authors.forename: Christopher J
authors.initials: CJ
authors.lastname: Schofield
mesh_terms: D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D006860:Hydrogen Bonding; D006877:Hydroxamic Acids / Q000138:chemical synthesis* / Q000494:pharmacology*; D007202:Indicators and Reagents; D008024:Ligands; D008958:Models, Molecular; D008968:Molecular Conformation; D013329:Structure-Activity Relationship; D065093:beta-Lactamase Inhibitors; D001618:beta-Lactamases
chemical_list: D004791:Enzyme Inhibitors; D006877:Hydroxamic Acids; D007202:Indicators and Reagents; D008024:Ligands; D065093:beta-Lactamase Inhibitors; C434285:beta-lactamase FEZ-1; D001618:beta-Lactamases