TY - JOUR
T1 - Chemotherapeutic activity of clofazimine and its analogues against Mycobacterium tuberculosis
T2 - In vitro, intracellular, and in vivo studies
AU - Jagannath, Chinnaswamy
AU - Reddy, M. Venkata
AU - Kailasam, Subramanian
AU - O'Sullivan, J. F.
AU - Gangadharam, Pattisapu R.J.
PY - 1995/4
Y1 - 1995/4
N2 - 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.
AB - 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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U2 - 10.1164/ajrccm.151.4.7697235
DO - 10.1164/ajrccm.151.4.7697235
M3 - Article
C2 - 7697235
AN - SCOPUS:0028933435
VL - 151
SP - 1083
EP - 1086
JO - American journal of respiratory and critical care medicine
JF - American journal of respiratory and critical care medicine
SN - 1073-449X
IS - 4
ER -