[In vitro and in vivo activities of newly synthesized fluoroquinolones WQ-3345 and WQ-3402 against Mycobacterium leprae].
Activities of newly synthesized fluoroquinolnes WQ-3345 and WQ-3402 against M. leprae were measured by using the Buddemeyer method. The % inhibition of the examined drugs for M. leprae was in the order of RFP > WQ-3402 > SPFX > GFLX > WQ-3345 > LVFX. The anti-M. leprae activity of WQ-3402 was found to be strongest in these five fluoroquinolones when examined by this method, and the activity of WQ-3345 was weaker than that of GFLX. The anti-M. leprae activities of WQ-3345 and WQ-3402 were measured by a mouse footpad method using nude mice. The inhibitory effects on the growth of M. leprae inoculated into the footpads were found to be incomplete after orally administered with WQ-3345 or WQ-3402 respectively at dosages of 10 and 20 mg/kg, and the incomplete inhibition was again was again found even at a dosage of 30, 40, or 50 mg/kg im the latter.
Gidoh
Masaichi
M
Leprosy Research Center, National institute of Infectious Diseases 4-2-1, Aoba-cho, Higashimurayama-shi, Tokyo 189-0002, Japan. m-gidoh@nih.go.jp
D000818:Animals; D004305:Dose-Response Relationship, Drug; D024881:Drug Resistance, Bacterial; D005260:Female; D024841:Fluoroquinolones / Q000494:pharmacology*; D006614:Hindlimb / Q000382:microbiology; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D008819:Mice, Nude; D009166:Mycobacterium leprae / Q000187:drug effects*
C500724:1-(5-amino-2,4-difluorophenyl)-6-fluoro-8-methyl-7-methylamino-4-oxo-1,4-dihydroquinoline-3-carboxylic acid; C500725:7-amino-1-(5-amino-2,4-difluorophenyl)-6-fluoro-8-methyl-4-oxo-1,4-dihydroquinoline-3-carboxylic acid; D024841:Fluoroquinolones