title: The synthesis and SAR of rhodanines as novel class C beta-lactamase inhibitors.
abstract: Beta-lactam antibiotics such as the cephalosporins and penicillins have diminished clinical effectiveness due to the hydrolytic activity of diverse beta-lactamases, especially those in molecular classes A and C. A structure activity relationship (SAR) study of a high-throughput screening lead resulted in the discovery of a potent and selective non-beta-lactam inhibitor of class C beta-lactamases.
authors.affiliation: Antimicrohial Agents Research, The R. W. Johnson Pharmaceutical Research Institute, Raritan, NJ 08869, USA. egrant@prius.jnj.com
authors.forename: E B
authors.initials: EB
authors.lastname: Grant
authors.forename: D
authors.initials: D
authors.lastname: Guiadeen
authors.forename: E Z
authors.initials: EZ
authors.lastname: Baum
authors.forename: B D
authors.initials: BD
authors.lastname: Foleno
authors.forename: H
authors.initials: H
authors.lastname: Jin
authors.forename: D A
authors.initials: DA
authors.lastname: Montenegro
authors.forename: E A
authors.initials: EA
authors.lastname: Nelson
authors.forename: K
authors.initials: K
authors.lastname: Bush
authors.forename: D J
authors.initials: DJ
authors.lastname: Hlasta
mesh_terms: D004353:Drug Evaluation, Preclinical; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D015394:Molecular Structure; D010878:Piperacillin / Q000037:antagonists & inhibitors / Q000494:pharmacology; D012236:Rhodanine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship; D065093:beta-Lactamase Inhibitors; D001618:beta-Lactamases / Q000145:classification
chemical_list: D004791:Enzyme Inhibitors; D065093:beta-Lactamase Inhibitors; D012236:Rhodanine; D001618:beta-Lactamases; D010878:Piperacillin