Mandell W, Neu H C
Antimicrob Agents Chemother. 1986 May;29(5):852-7. doi: 10.1128/AAC.29.5.852.
The in vitro activity of CI-934, a new 4-quinolone, was determined against gram-positive and gram-negative bacteria. The MICs for 90% of the isolates tested were 0.25 microgram/ml for Streptococcus pneumoniae, 0.5 microgram/ml for Streptococcus faecalis, 0.25 microgram/ml for staphylococci, including methicillin-resistant strains, and less than or equal to 1.0 microgram/ml for Escherichia coli, Salmonella and Shigella spp., Klebsiella spp., Proteus spp., and Citrobacter spp. CI-934 had activity superior to that of other quinolones against streptococci by four- to eightfold. Against members of the family Enterobacteriaceae, ciprofloxacin was 2- to 18-fold more active; ofloxacin and norfloxacin were twofold more active or similar to CI-934. CI-934 inhibited ampicillin-cephalothin-resistant urinary isolates of E. coli, Klebsiella pneumoniae, and Proteus mirabilis and cefoxatime-resistant Acinetobacter spp., Citrobacter freundii, Enterobacter cloacae, Proteus vulgaris, and Morganella morganii. The medium, inoculum size, and oxygen concentration, as well as the addition of serum, had not major effect on the activity of CI-934. Magnesium at a concentration of 9 mM increased MICs and MBCs four- to eightfold, and testing at pH 6 increased MICs as much as 32- to 64-fold for some organisms in comparison with MICs at pH 7. The frequency of spontaneous mutation to resistance was comparable to that for other new quinolones, but resistant isolates could be selected by repeated subculture.
新型4-喹诺酮类药物CI-934对革兰氏阳性菌和革兰氏阴性菌的体外活性进行了测定。受试的90%分离株的最低抑菌浓度(MIC)分别为:肺炎链球菌0.25微克/毫升,粪肠球菌0.5微克/毫升,葡萄球菌(包括耐甲氧西林菌株)0.25微克/毫升,大肠杆菌、沙门氏菌、志贺氏菌属、克雷伯氏菌属、变形杆菌属和柠檬酸杆菌属小于或等于1.0微克/毫升。CI-934对链球菌的活性比其他喹诺酮类药物高4至8倍。对肠杆菌科成员,环丙沙星的活性高2至18倍;氧氟沙星和诺氟沙星的活性高2倍或与CI-934相似。CI-934抑制了对氨苄西林-头孢噻吩耐药的大肠杆菌、肺炎克雷伯菌和奇异变形杆菌的尿液分离株,以及对头孢西丁耐药的不动杆菌属、弗氏柠檬酸杆菌、阴沟肠杆菌、普通变形杆菌和摩根氏摩根菌。培养基、接种量、氧浓度以及血清的添加对CI-934的活性没有重大影响。9毫摩尔浓度的镁使MIC和MBC增加4至8倍,与pH 7时的MIC相比,在pH 6下测试使某些生物体的MIC增加多达32至64倍。自发耐药突变的频率与其他新型喹诺酮类药物相当,但耐药分离株可通过反复传代培养来筛选。