Tsuchimori N, Okonogi K
Takeda Chemical Industries Ltd, Osaka 532, Japan.
J Antimicrob Chemother. 1996 Mar;37(3):605-9. doi: 10.1093/jac/37.3.605.
The concentration of cefozopran which inhibits binding of [14C]benzylpenicillin to penicillin-binding protein (PBP) 5 of Enterococcus faecalis TN2OO5 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 TN2OO5 by binding to PBP 5.
抑制[14C]苄青霉素与粪肠球菌TN2OO5的青霉素结合蛋白（PBP）5结合50%时头孢唑啉的浓度为11 mg/L，其MIC为12.5 mg/L。头孢他啶和头孢甲肟在100 mg/L时无活性，在此浓度下对PBP 5无亲和力。氨苄西林、苄青霉素和亚胺培南对PBPs 3/4和PBP 5的亲和力高于头孢唑啉，且它们的MIC低于头孢唑啉。未发现受试化合物的MIC与对PBP 1、2或6的亲和力之间存在相关性。这些结果表明，头孢唑啉通过与PBP 5结合而对粪肠球菌TN2OO5表现出抗菌活性。
