In vivo activities of novel benzoxazinorifamycins against Mycobacterium leprae.
Among the four newly synthesized benzoxazinorifamycin derivatives, KRM-1648 and KRM-2312 completely inhibited the multiplication of rifampicin-sensitive as well as rifampicin-resistant strains of M. leprae in the foot-pads of mice. Both were found to be more potent than rifampicin and were bactericidal. In combination with ofloxacin, another potent bactericidal drug against M. leprae, both KRM-1648 and KRM-2312 exhibited synergism. Thus, combination of one of these benzoxazinorifamycin derivatives and ofloxacin in multidrug regimens is worth evaluating in clinical trials.
Dhople
A M
AM
Biological Sciences, Florida Institute of Technology, Melbourne 32901, USA.
Ibanez
M A
MA
D000818:Animals; D007917:Leprostatic Agents / Q000494:pharmacology*; D051379:Mice; D008807:Mice, Inbred BALB C; D009166:Mycobacterium leprae / Q000187:drug effects*; D012294:Rifamycins / Q000494:pharmacology*
D007917:Leprostatic Agents; D012294:Rifamycins; C068980:KRM 1648