Barrett M S, Jones R N, Erwin M E
Department of Pathology, University of Iowa College of Medicine, Iowa City 52242.
Eur J Clin Microbiol Infect Dis. 1993 Feb;12(2):134-41. doi: 10.1007/BF01967592.
The compound E-4868 (Laboratorios Dr. Esteve) is a trifluoro, 7-azetidinyl quinolone with properties resembling those of other fluoroquinolones. Its activity in vitro was compared to that of six other similar drugs against more than 700 nosocomial isolates using standard methods. The MIC50s of E-4868 for enteric bacilli ranged from 0.015 to 0.25 micrograms/ml, being highest for Providencia spp. Pseudomonas aeruginosa strains were two-fold more susceptible to E-4868 than to ofloxacin. MICs of E-4868 for Haemophilus influenzae, Moraxella catarrhalis and pathogenic Neisseria spp. were all < or = 0.12 micrograms/ml. E-4868 was equal in activity to or eight-fold more active than ciprofloxacin against gram-positive cocci. The MICs of E-4868 for pneumococci were all < or = 0.5 micrograms/ml but anaerobes such as Bacteroides fragilis were generally less susceptible (MIC90, 4 micrograms/ml). There was almost complete cross-resistance to several other fluoroquinolones. Resistant mutants were selected by a multiple passage technique but the rate of mutation to resistance was very low (< 10(-8)) at an 8 x MIC.
化合物E - 4868（埃斯特维博士实验室）是一种三氟7 - 氮杂环丁烷基喹诺酮，其性质与其他氟喹诺酮类药物相似。使用标准方法，将其体外活性与其他六种类似药物针对700多种医院分离株的活性进行了比较。E - 4868对肠道杆菌的MIC50范围为0.015至0.25微克/毫升，对普罗威登斯菌属最高。铜绿假单胞菌菌株对E - 4868的敏感性比对氧氟沙星高两倍。E - 4868对流感嗜血杆菌、卡他莫拉菌和致病性奈瑟菌属的MIC均≤0.12微克/毫升。E - 4868对革兰氏阳性球菌的活性与环丙沙星相当或比其高八倍。E - 4868对肺炎球菌的MIC均≤0.5微克/毫升，但脆弱拟杆菌等厌氧菌通常敏感性较低（MIC90为4微克/毫升）。对其他几种氟喹诺酮类药物几乎完全交叉耐药。通过多次传代技术筛选出耐药突变体，但在8倍MIC浓度下，耐药突变率非常低（<10^(-8)）。
