CP-45,899, a Beta-Lactamase Inhibitor That Extends the Antibacterial Spectrum of Beta-Lactams: Initial Bacteriological Characterization

摘要: CP-45,899 {3,3-dimethyl-7-oxo-4-thia-1-azabicyclo(3.2.0)heptane-2-carboxylic acid, 4,4-dioxide, [2S-(2α,5α)]} is an irreversible inhibitor of several bacterial penicillinases and cephalosporinases. In the presence low concentrations CP-45,899, ampicillin other β-lactams readily inhibit growth a variety resistant bacteria that contain β-lactamases. used alone displays only weak antibacterial activity, with notable exception its potent effects on susceptible strains Neisseria gonorrhoeae . appears to be somewhat less but markedly more stable (in aqueous solution) than recently described β-lactamase clavulanic acid. The spectrum extensions provided by two compounds are similar. A 1:1 mixture marked antimicrobial activity in mice experimentally infected ampicillin-resistant Staphylococcus aureus, Haemophilus influenzae, Klebsiella pneumoniae , Proteus vulgaris