两种口服头孢菌素代谢产物Ro 15 - 8074和Ro 19 - 5247的体外活性
In vitro activity of Ro 15-8074 and Ro 19-5247, two orally administered cephalosporin metabolites.
作者信息
Wise R, Andrews J M, Piddock L J
出版信息
Antimicrob Agents Chemother. 1986 Jun;29(6):1067-72. doi: 10.1128/AAC.29.6.1067.
Abstract
The activity of two iminomethoxy aminothiazoly cephalosporins, Ro 15-8074 and Ro 19-5247, was compared with that of other beta-lactams against a total of 491 bacterial strains. Both were highly active (MIC for 90% of the strains tested [MIC 90], less than or equal to 2 micrograms/ml) against the majority of the members of the family Enterobacteriaceae, Haemophilus influenzae, Neisseria spp., and Streptococcus pneumoniae, being at least 16-fold more active than cephalexin and 8-fold more active than cefuroxime. There was no activity against Pseudomonas aeruginosa and poor activity against Morganella morganii (in the case of Ro 15-8074), Enterobacter sp., and Citrobacter sp. Staphylococcus aureus was moderately susceptible to Ro 19-5247 (MIC90, 8 micrograms/ml), but Ro 15-8074 was eightfold less active. The protein binding of the two compounds at 5 micrograms/ml was 9.1% for Ro 15-8074 and 69.9% for Ro 19-5247. The major target site for the two cephalosporins was PBP 3.
摘要
将两种亚胺甲氧基氨基噻唑头孢菌素Ro 15 - 8074和Ro 19 - 5247与其他β-内酰胺类药物对总共491株细菌的活性进行了比较。二者对大多数肠杆菌科细菌、流感嗜血杆菌、奈瑟菌属和肺炎链球菌均具有高活性（90%受试菌株的最低抑菌浓度[MIC90]≤2微克/毫升），其活性至少比头孢氨苄高16倍，比头孢呋辛高8倍。对铜绿假单胞菌无活性，对摩根摩根菌（Ro 15 - 8074的情况）、阴沟肠杆菌和柠檬酸杆菌活性较差。金黄色葡萄球菌对Ro 19 - 5247中度敏感（MIC90，8微克/毫升），但Ro 15 - 8074的活性低8倍。两种化合物在5微克/毫升时的蛋白结合率，Ro 15 - 8074为9.1%，Ro 19 - 5247为69.9%。这两种头孢菌素的主要作用靶点是PBP 3。
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