Synthesis of new verapamil analogues and their evaluation in combination with rifampicin against Mycobacterium tuberculosis and molecular docking studies in the binding site of efflux protein Rv1258c

Kawaljit Singh, Malkeet Kumar, Elumalai Pavadai, Krupa Naran, Digby F. Warner, Peter G. Ruminski, Kelly Chibale

Research output: Contribution to journalArticle

19 Scopus citations

Abstract

New verapamil analogues were synthesized and their inhibitory activities against Mycobacterium tuberculosis H37Rv determined in vitro alone and in combination with rifampicin (RIF). Some analogues showed comparable activity to verapamil and exhibited better synergies with RIF. Molecular docking studies of the binding sites of Rv1258c, a M. tuberculosis efflux protein previously implicated in intrinsic resistance to RIF, suggested a potential rationale for the superior synergistic interactions observed with some analogues.

Original languageEnglish
Pages (from-to)2985-2990
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Volume24
Issue number14
DOIs
StatePublished - Jul 15 2014
Externally publishedYes

Keywords

  • Efflux pump
  • Rifampicin
  • Rv1258c
  • Tuberculosis
  • Verapamil

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