Espinoza A M, Chin N X, Novelli A, Neu H C
Department of Medicine, College of Physicians & Surgeons, Columbia University, New York, New York 10032.
Antimicrob Agents Chemother. 1988 May;32(5):663-70. doi: 10.1128/AAC.32.5.663.
The in vitro activity of a new quinolone, T-3262 [A-60969; DL-7-(3-amino-1-pyrrolidinyl)-1-(2,4-difluorophenyl)-6-fluoro-1-, 4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acid monohydrate], was compared with those of ciprofloxacin, ofloxacin, ceftazidime, imipenem, and gentamicin. T-3262 inhibited 90% of isolates of the family Enterobacteriaceae at a concentration of less than or equal to 0.25 micrograms/ml. It was two to four times more active than ofloxacin and similarly or slightly less active than ciprofloxacin. Ninety percent of isolates of Pseudomonas aeruginosa were inhibited at 0.5 micrograms/ml. It was 4- to 8-fold more active than ciprofloxacin and 8- to 16-fold more active than ofloxacin against Pseudomonas cepacia and Pseudomonas maltophilia, which were resistant to imipenem and gentamicin. Most Haemophilus influenzae, Neisseria gonorrhoeae, and Branhamella catarrhalis isolates were inhibited at concentrations of less than or equal to 0.008 micrograms/ml. The MIC for 90% of the Staphylococcus aureus isolates, including methicillin-resistant S. aureus, was 0.12 micrograms/ml; that for Staphylococcus epidermidis was 0.5 micrograms/ml, as was that for Enterococcus faecalis. It inhibited 90% of Bacteroides fragilis isolates at 2 micrograms/ml, considerably more active than ciprofloxacin and ofloxacin. The frequency of spontaneous point mutational resistance was less than 10(-10) for members of the family Enterobacteriaceae and Pseudomonas spp. Resistant strains could be selected by repeated subculture. Similar to other quinolones, its activity could be affected by culture conditions. T-3262 showed a postantibiotic suppressive effect on Escherichia coli, P. aeruginosa, and S. aureus.
将一种新型喹诺酮类药物T-3262 [A-60969；DL-7-(3-氨基-1-吡咯烷基)-1-(2,4-二氟苯基)-6-氟-1,4-二氢-4-氧代-1,8-萘啶-3-羧酸一水合物] 的体外活性与环丙沙星、氧氟沙星、头孢他啶、亚胺培南和庆大霉素进行了比较。T-3262在浓度小于或等于0.25微克/毫升时可抑制90% 的肠杆菌科细菌分离株。其活性比氧氟沙星高2至4倍，与环丙沙星活性相似或略低。90% 的铜绿假单胞菌分离株在0.5微克/毫升时被抑制。对于对亚胺培南和庆大霉素耐药的洋葱伯克霍尔德菌和嗜麦芽窄食单胞菌，它的活性比环丙沙星高4至8倍，比氧氟沙星高8至16倍。大多数流感嗜血杆菌、淋病奈瑟菌和卡他莫拉菌分离株在浓度小于或等于0.008微克/毫升时被抑制。包括耐甲氧西林金黄色葡萄球菌在内的90% 的金黄色葡萄球菌分离株的最低抑菌浓度为0.12微克/毫升；表皮葡萄球菌和粪肠球菌的最低抑菌浓度为0.5微克/毫升。它在2微克/毫升时可抑制90% 的脆弱拟杆菌分离株，活性明显高于环丙沙星和氧氟沙星。肠杆菌科细菌和假单胞菌属成员的自发点突变耐药频率小于10(-10)。通过反复传代可筛选出耐药菌株。与其他喹诺酮类药物相似，其活性可能受培养条件影响。T-3262对大肠杆菌、铜绿假单胞菌和金黄色葡萄球菌表现出抗生素后效应。
