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Journal of Antimicrobial Chemotherapy (1996) 37, 605-609
© 1996 The British Society for Antimicrobial Chemotherapy

brief-report

Penicillin-binding protein 5 as an inhibitory target of cefozopran in Enterococcus faecalis

Noboru Tsuchimori and Kenji Okonogi

Pharmaceutical Research Laboratories III, Takeda Chemical Industries Ltd 2-17-85 Jusohonmachi, Yodogawa-ku, Osaka 532, Japan

Received 5 May 1995; returned 5 July 1995; accepted 2 October 1995

The concentration of cefozopran which inhibits binding of [14C]benzylpenicillin to penicillin-binding protein (PBP) 5 of Enterococcus faecalis TN2005 by 50% was 11 mg/L, and its MIC was 12.5 mg/L. Ceftazidime and cefmenoxime, which were inactive at 100 mg/L, showed no affinity for PBP 5 at this concentration. Ampicillin, benzylpenicillin and imipenem showed higher affinity for PBPs 3/4 and PBP 5 than cefozopran, and their MICs were lower than that of cefozopran. No correlation between MICs of the test compounds and the affinity for PBP 1, 2 or 6 was found. These results suggest that cefozopran exhibits antimicrobial activity against E. faecalis TN2005 by binding to PBP 5.


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