Synthesis and structure activity relationship of imidazo[1,2-a]pyridine-8-carboxamides as a novel antimycobacterial lead series

Bioorg Med Chem Lett. 2013 Sep 1;23(17):4996-5001. doi: 10.1016/j.bmcl.2013.06.043. Epub 2013 Jun 24.

Abstract

Imidazo[1,2-a]pyridine-8-carboxamides as a novel antimycobacterial lead were generated by whole cell screening of a focused library against Mycobacterium tuberculosis. Herein, we describe the synthesis and structure activity relationship evaluation of this class of inhibitors and the optimization of physicochemical properties. These are selective inhibitors of Mycobacterium tuberculosis with no activity on either gram positive or gram negative pathogens.

Keywords: Antimycobacterial activity; Physicochemical properties; Structure activity relationship; Whole cell screening.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amides / chemistry
  • Amides / pharmacology
  • Antitubercular Agents / chemistry*
  • Antitubercular Agents / pharmacology*
  • Humans
  • Microbial Sensitivity Tests
  • Models, Molecular
  • Mycobacterium tuberculosis / drug effects*
  • Pyridines / chemistry*
  • Pyridines / pharmacology*
  • Structure-Activity Relationship
  • Tuberculosis / drug therapy

Substances

  • Amides
  • Antitubercular Agents
  • Pyridines
  • imidazo(1,2-a)pyridine