COMPARATIVE INVITRO ACTIVITIES OF 20 FLUOROQUINOLONES AGAINST MYCOBACTERIUM-LEPRAE
COMPARATIVE INVITRO ACTIVITIES OF 20 FLUOROQUINOLONES AGAINST MYCOBACTERIUM-LEPRAE
复制标题
DOI：
10.1128/aac.34.2.229
复制
发表时间：
1990-02-01
影响因子：
4.9
通讯作者：
WHITE, KE
中科院分区：
文献类型：
--
作者：
FRANZBLAU, SG;WHITE, KE
采用BACTEC 460系统评价了20种氟喹诺酮类药物对麻风分枝杆菌的体外抗菌活性。M.在0.31 - 5 μ g/ml的氟喹诺酮存在下，将麻风在BACTEC 12 B培养基中于33 ℃、低氧下孵育2 - 3周。通过与无药物对照相比14 CO2释放的减少来确定活性。在市售药物中，氧氟沙星活性最高，而依诺沙星和诺氟沙星无活性。然而，许多较新的氟喹诺酮类药物（AT-4140、OPC-17100、OPC-17066、PD-117596、PD-124816、PD-127391和WIN-57273），除WIN-57273外，均在R-1处含有环丙基，在R-8处含有卤素或甲基，在体外比氧氟沙星更有活性。对这些药物的进一步体内评价应有助于确定其用于治疗麻风病的潜力。
The in vitro activities of 20 fluoroquinolones against Mycobacterium leprae were evaluated by using the BACTEC 460 system. M. leprae was incubated in BACTEC 12B medium at 33.degree.C under reduced oxygen for 2 to 3 weeks in the presence of fluoroquinolones at 0.31 to 5 .mu.g/ml. Activity was determined by a reduction in 14CO2 evolution compared with that of drug-free controls. Of the commercially available agents, ofloxacin was most active, while enoxacin and norfloxacin were inactive. However, a number of newer fluorquinolones (AT-4140, OPC-17100, OPC-17066, PD-117596, PD-124816, PD-127391, and WIN-57273), all containing a cyclopropyl group at R-1 and, with the exception of WIN-57273, either a halogen or methyl group at R-8, were more active than ofloxacin in vitro. Further in vivo evaluations of these agents should help determine their potential for use against leprosy.