Synthesis and preliminary biological evaluation of novel N-(3-aryl-1,2,4-triazol-5-yl) cinnamamide derivatives as potential antimycobacterial agents: an operational Topliss Tree approach

  • Bioorg Med Chem Lett. 2011 Nov 1;21(21):6523-6. doi: 10.1016/j.bmcl.2011.08.076.
Manoj D Kakwani  1 ,  Nutan H Palsule Desai ,  Arundhati C Lele ,  Muktikant Ray ,  M G R Rajan ,  Mariam S Degani
Affiliations
  • 1. Institute of Chemical Technology, Nathalal Parekh Marg, Matunga, Mumbai 400 019, India.
PMID: 21917452 DOI: 10.1016/j.bmcl.2011.08.076
Abstract

A series of novel N-(3-aryl-1,2,4-triazol-5-yl) cinnamamide derivatives were designed on basis of structural similarity to the known FAS II inhibitors. Topliss operational method was used to optimize the potency of molecules. The minimum inhibitory concentration (MIC) of all synthesized compounds was determined against Mycobacterium tuberculosis H(37)R(v) using resazurin microtitre assay (REMA) plate method. The synthesized compounds exhibit antimycobacterial activity in the range of 5-95μM with a good safety profile.