Synthesis and beta-lactamase inhibitory activities of some clavulanic acid analogues.
Clavulanic acid analogs lacking the C-3 carboxyl group are potent inhibitors of both plasmid and chromosomally mediated beta-lactamases. They exhibit only low intrinsic anti-bacterial activity, but potentiate the activity of ampicillin and cephaloridine against beta-lactamase producing Escherichia coli and Enterobacter cloacae in vitro. No synergism was observed in beta-lactamase negative strains. The E. coli TEM 1 and the E. cloacae P99 enzymes are inhibited in a progressive and irreversible manner by these compounds.
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects; D019818:Clavulanic Acid; D002969:Clavulanic Acids / Q000494:pharmacology; D004357:Drug Synergism; D007700:Kinetics; D013329:Structure-Activity Relationship; D065093:beta-Lactamase Inhibitors
D000900:Anti-Bacterial Agents; D002969:Clavulanic Acids; D065093:beta-Lactamase Inhibitors; D019818:Clavulanic Acid