@article{5685, keywords = {Animals, Antibiotics, Antitubercular, Female, Mice, Mice, Inbred BALB C, Mice, Nude, Mycobacterium leprae, Rifampin, Rifamycins}, author = {Gidoh M and Tsutsumi S and Yamane T and Yamashita K and Hosoe K and HIDAKA T}, title = {Bactericidal action at low doses of a new rifamycin derivative, 3'-hydroxy-5'-(4-isobutyl-1-piperazinyl) benzoxazinorifamycin (KRM-1648) on Mycobacterium leprae inoculated into footpads of nude mice.}, abstract = {

Among a series of newly-synthesized benzoxazinorifamycins, 2 of the 3'-hydroxy-5'-(4-alkyl-1-piperazinyl) derivatives, named KRM-1648 and KRM-2312, whose respective alkyl residues are isobutyl and isopropyl, were examined for efficacy against nude mouse-model leprosy. KRM-1648 completely inhibited the growth of leprosy bacilli inoculated into nude mouse footpads, even 6 months after the medication had been stopped, when given orally at a daily dose of 0.6 mg/kg, 5 or 6 times weekly, during 3-5 months postinoculation. In comparison, the growth inhibition by KRM-2312 was incomplete under the same conditions, though it was still stronger than that by rifampicin. Complete growth inhibition by KRM-1648 was also observed when it was given orally at a dose of 1 or 3 mg/kg twice weekly during the same period. In contrast, the growth inhibition by rifampicin was only slight at 1 mg/kg and partial at 3 mg/kg under the same condition.

}, year = {1992}, journal = {Leprosy review}, volume = {63}, pages = {319-28}, month = {1992 Dec}, issn = {0305-7518}, url = {http://leprev.ilsl.br/pdfs/1992/v63n4/pdf/v63n4a03.pdf}, language = {eng}, }