文章基本信息

标题：CW-270033, a Novel Pyrrolidinyl-thio Carbapenem, Has Potent Antimicrobial Activity in Vitro and in Vivo
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作者：JongMyeung Kim ; Jong Ryul Ha ; Se Woong Oh 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：2007
卷号：30
期号：3
页码：575-579
DOI：10.1248/bpb.30.575
出版社：The Pharmaceutical Society of Japan
摘要：CW-270033, an injectable carbapenem, is a novel, synthesized pyrrolidinyl-thio carbapenem. In the present study, the in-vitro and in-vivo antibacterial activities of CW-270033 against wild-type strains and clinical isolates were compared with those of imipenem and meropenem. CW-270033 was more active than imipenem against Gram-negative ( Escherichia coli and Pseudomonas aeruginosa ) clinical isolates, but was slightly less active than meropenem. Against the Gram-positive clinical isolates methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococcus (VRE), CW-270033 was slightly more active than meropenem, but was less active than imipenem. CW-270033 displayed potent in-vivo activity against E. coli ATCC 25922, P. aeruginosa ATCC 27853, and S. aureus S MITH in the mouse systemic infection model; the efficacy of CW-270033 in this model was 2—7 fold higher than that of meropenem. This activity was comparable to the in-vitro activity of CW-270033. An intravenous injection of CW-270033 showed that the half-life of CW-270033 in serum in mice was about 20 min, which was about two times that of meropenem. CW-270033 was also found to be resistant to hydrolysis by the mouse renal dehydropeptidase I (DHP-I) enzyme.
关键词：carbapenem;CW-270033;minimum inhibitory concentration (MIC);protection test;dehydropeptidase I