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- Title
In-vitro and in-vivo antimicrobial activities of a novel cephalosporin derivative, CP6162, possessing a dihydroxypyridone moiety at the C-3 side chain.
- Authors
Orikasa, Yoshinori; Hara, Tetsuro; Miyata, Aiko; Tamura, Atsushi; Kawaharajo, Katsumi; Matsumoto, Takashi; Komiya, Izumi; Iwamatsu, Katsuyoshi; Shibahara, Seiji; Inouye, Shigeharu; Orikasa, Y; Hara, T; Miyata, A; Tamura, A; Kawaharajo, K; Matsumoto, T; Komiya, I; Iwamatsu, K; Shibahara, S; Inouye, S
- Abstract
The antibacterial activity of a novel cephalosporin derivative, CP6162, possessing a dihydroxypyridone moiety at the C-3 side chain, was evaluated in vitro and in vivo, with ceftazidime, aztreonam and cefoperazone as the reference antibiotics. CP6162 showed weak or little activity against Gram-positive bacteria, but potent activity against clinical isolates of the Gram-negative species including strains of Pseudomonas aeruginosa, Ps. cepacia, Acinetobacter sp., Xanthomonas maltophilia, Serratia marcescens, Enterobacter cloacae and Citrobacter freundii, which were resistant to the reference antibiotics. The MICs of CP6162 were only slightly affected by the high producers of beta-lactamases except for cephalosporinase-producing C. freundii. It was, however, affected by the presence of ferric ion. CP6162 showed in-vivo activity paralleling the in-vitro activity, and also showed pharmacokinetic parameters similar to those of ceftazidime in mice and rats.
- Subjects
ANIMAL experimentation; AZTREONAM; CEFOPERAZONE; CEPHALOSPORINS; COMPARATIVE studies; DRUG design; CLINICAL drug trials; GRAM-negative bacteria; GRAM-positive bacteria; HYDROLASES; MICE; RATS; CEFTAZIDIME; PHARMACODYNAMICS
- Publication
Journal of Antimicrobial Chemotherapy (JAC), 1991, Vol 27, Issue 1, p41
- ISSN
0305-7453
- Publication type
journal article