CHEMOTHERAPEUTIC ACTIVITY OF CLOFAZIMINE AND ITS ANALOGS AGAINST MYCOBACTERIUM-TUBERCULOSIS - IN-VITRO, INTRACELLULAR, AND IN-VIVO STUDIES

Clofazimine (CFM), a riminophenazine drug, is primarily used in therap y for leprosy and Mycobacterium avium infections. With an objective of identifying drugs active against Mycobacterium tuberculosis, includin g those with multi-drug resistance, we investigated CFM and nine of it s chemical analogues. Among these, B746 and B4101 had better activity than CFM against six drug-susceptible and nine single/multiple drug-re sistant M. tuberculosis strains. B746 also showed slightly better acti vity than CFM against intracellular M. tuberculosis in J774A.1 macroph ages and was comparable to CFM in its in vivo activity against experim ental tuberculosis in C57BL/6 mice. Interestingly, it caused less pigm entation in internal organs.