The synthesis and SAR of rhodanines as novel class C beta-lactamase inhibitors.
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.
Grant
E B
EB
Antimicrohial Agents Research, The R. W. Johnson Pharmaceutical Research Institute, Raritan, NJ 08869, USA. egrant@prius.jnj.com
Guiadeen
D
D
Baum
E Z
EZ
Foleno
B D
BD
Jin
H
H
Montenegro
D A
DA
Nelson
E A
EA
Bush
K
K
Hlasta
D J
DJ
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
D004791:Enzyme Inhibitors; D065093:beta-Lactamase Inhibitors; D012236:Rhodanine; D001618:beta-Lactamases; D010878:Piperacillin