01751nas a2200313   4500000000100000008004100001260001300042653002500055653001200080653002700092653003700119653001100156653002300167653001200190653000900202653002400211653001500235653002500250653001300275653001500288100001400303700001200317245009000329856004100419300001000460490000700470520094600477022001401423       1993                            d  c1993 Jun10aAdministration, Oral10aAnimals10aDisease Models, Animal10aDose-Response Relationship, Drug10aFemale10aLeprostatic Agents10aleprosy10aMice10aMice, Inbred BALB C10aMice, Nude10aMycobacterium leprae10aRifampin10aRifamycins1 aTomioka H1 aSaito H00aIn vivo antileprosy activity of the newly synthesized benzoxazinorifamycin, KRM-1648.  uhttp://ila.ilsl.br/pdfs/v61n2a11.pdf  a255-80 v613 a<p>The in vivo anti-Mycobacterium leprae activity of the newly synthesized benzoxazinorifamycin, KRM-1648, was studied. KRM-1648 was given orally to athymic nude mice, infected subcutaneously with M. leprae in the hindfoot pad, at doses between 0.001 and 0.01 mg of the drug/mouse/day six times per week, from day 31 to day 80. KRM-1648 administration markedly suppressed bacterial growth in the foot pads for 360 days. KRM-1648 given daily at the dose of 0.01 mg/mouse elicited a 2-4-log decrease in the number of acid-fast bacilli. The therapeutic effects of KRM-1648 were significantly higher than that of rifampin when both drugs were given in the same dosage. Moreover, when mice were fed a KRM-1648-containing diet (0.00004%-0.0004%), the drug displayed an even higher efficacy against M. leprae infection, causing an almost 4-log decrease in the number of leprosy bacilli in the infected foot pad compared to untreated controls.</p>
  a0148-916X