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- SHIGI YASUTAKA
- Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.
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- MATSUMOTO YOSHIMI
- Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.
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- KAIZU MAMIKO
- Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.
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- FUJISHITA YOKO
- Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.
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- KOJO HITOSHI
- Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.
抄録
The mechanism of action of a new orally active cephalosporin, FK027, was compared to that of cephalexin and cefaclor to elucidate its excellent antibacterial activity against Gram-negative bacteria. FK027 showed very high affinity for the penicillin-binding proteins (PBPs) 3, 1a and 1bs of Escherichia coli whereas cephalexin showed fairly high affinity for PBPs 1a, 4 and 3. The ability of FK027 to penetrate the outer membranes of E. coli and Enterobacter cloacae was less than that of cephalexin and cefaclor. However, FK027 was extremely stable to both plasmid-mediated penicillinases and chromosomal β-lactamases except theBacteroides fragilis enzyme and its stability was superior to that of cephalexin and cefaclor. These results indicate that the potent antibacterial activity of FK027 is based on its enhanced affinity for the target enzymes and its high stability to β-lactamases.
収録刊行物
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- The Journal of Antibiotics
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The Journal of Antibiotics 37 (7), 790-796, 1984
公益財団法人 日本感染症医薬品協会
