Chemotherapeutic activity of clofazimine and its analogues against Mycobacterium tuberculosis: In vitro, intracellular, and in vivo studies

Chinnaswamy Jagannath, M. Venkata Reddy, Subramanian Kailasam, J. F. O'Sullivan, Pattisapu R.J. Gangadharam

Research output: Contribution to journalArticlepeer-review

77 Scopus citations

Abstract

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.

Original languageEnglish (US)
Pages (from-to)1083-1086
Number of pages4
JournalAmerican journal of respiratory and critical care medicine
Volume151
Issue number4
DOIs
StatePublished - Apr 1995
Externally publishedYes

ASJC Scopus subject areas

  • Pulmonary and Respiratory Medicine
  • Critical Care and Intensive Care Medicine

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