title: Comparative in vitro activities of 20 fluoroquinolones against Mycobacterium leprae.
abstract: 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 degrees C under reduced oxygen for 2 to 3 weeks in the presence of fluoroquinolones at 0.31 to 5 micrograms/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 fluoroquinolones (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.
authors.affiliation: Laboratory Research Branch, Gillis W. Long Hansen's Disease Center, Carville, Louisiana 70721.
authors.forename: S G
authors.initials: SG
authors.lastname: Franzblau
authors.forename: K E
authors.initials: KE
authors.lastname: White
mesh_terms: D042462:4-Quinolones; D000890:Anti-Infective Agents / Q000494:pharmacology*; D007917:Leprostatic Agents / Q000494:pharmacology*; D008826:Microbial Sensitivity Tests; D009166:Mycobacterium leprae / Q000187:drug effects*
chemical_list: D042462:4-Quinolones; D000890:Anti-Infective Agents; D007917:Leprostatic Agents