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The new quinolone WIN-57273 was shown to inhibit Staphylococcus aureus beta-lactamase activity noncompetitively in vitro with an apparent Ki value of 0.5 mM. MICs of penicillin G for a highly quinolone-resistant, beta-lactamase-negative strain in the presence of exogenous beta-lactamase decreased considerably when subinhibitory concentrations of WIN-57273 were added. Furthermore, the attachment transpeptidase reaction, investigated on whole cells of S. aureus, was impeded by WIN-57273 concentrations of greater than or equal to 30 microM. While these interactions suggest a novel mechanism of action for this compound, they are probably not relevant to the overall antibacterial potency of WIN-57273.

Citation

Y X Furet, C Lucain, J C Pechère. Relative beta-lactamase- and transpeptidase-inhibitory activities of the new quinolone WIN-57273 in Staphylococcus aureus. Antimicrobial agents and chemotherapy. 1992 Apr;36(4):894-7

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PMID: 1323958

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