01556nas a2200301 4500000000100000008004100001260001300042653001200055653001600067653001000083653000900093653000900102653002300111653003200134653003100166653001700197653003800214100001600252700001400268700001500282700001900297700002000316245014500336300001100481490000800492520074000500022001401240 1995 d c1995 Apr10aAnimals10aClofazimine10aLiver10aLung10aMice10aMice, Inbred C57BL10aMicrobial Sensitivity Tests10aMycobacterium tuberculosis10aTuberculosis10aTuberculosis, Multidrug-Resistant1 aJagannath C1 aReddy M V1 aKailasam S1 aO'Sullivan J F1 aGangadharam P R00aChemotherapeutic activity of clofazimine and its analogues against Mycobacterium tuberculosis. In vitro, intracellular, and in vivo studies. a1083-60 v1513 a

Clofazimine (CFM), a riminophenazine drug, is primarily used in therapy for leprosy and Mycobacterium avium infections. With an objective of identifying drugs active against Mycobacterium tuberculosis, including those with multi-drug resistance, we investigated CFM and nine of its chemical analogues. Among these, B746 and B4101 had better activity than CFM against six drug-susceptible and nine single/multiple drug-resistant M. tuberculosis strains. B746 also showed slightly better activity than CFM against intracellular M. tuberculosis in J774A.1 macrophages and was comparable to CFM in its in vivo activity against experimental tuberculosis in C57BL/6 mice. Interestingly, it caused less pigmentation in internal organs.

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