CP6679, a new injectable cephalosporin. Part 1: synthesis and structure-activity relationships |
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Authors: | Masakitsushima Iwamatsu K Umemura E Kudo T Sato Y Shiokawa S Takizawa H Kano Y Kobayashi K Ida T Tamura A Atsumi K |
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Institution: | Pharmaceutical Research Center, Meiji Seika Kaisha, Ltd., 760 Morooka-cho, Kohoku-ku, Yokohama 222–8567, Japan |
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Abstract: | A series of cephalosporins bearing a 5,5-fused ring system, an (imidazo5,1-b]thiazolium-6-yl)methyl group, at the C-3 position were synthesized and evaluated for in vitro antibacterial activities. CP6679 (1s) and its analogues showed potent antibacterial activities against Gram-positive and Gram-negative bacteria, including Pseudomonas aeruginosa. They were also highly active against methicillin-resistant Staphylococcus aureus (MRSA). CP6679 (1s) showed more potent antibacterial activity than ceftazidime (CAZ) or cefpirome (CPR) against Pseudomonas aeruginosa and MRSA. |
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