Synthesis and antitubercular screening of imidazole derivatives

Eur J Med Chem. 2009 Aug;44(8):3350-5. doi: 10.1016/j.ejmech.2009.02.013. Epub 2009 Feb 20.

Abstract

A series of imidazole based compounds were synthesized by reacting simple imidazoles with alkyl halides or alkyl halocarboxylate in presence of tetrabutylammonium bromide (TBAB). The compounds bearing carbethoxy group undergo amidation with different amines in the presence of DBU to give respective carboxamides. The synthesized compounds were screened against Mycobacterium tuberculosis where compound 17 exhibited very good in vitro antitubercular activity and may serve as a lead for further optimization.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antitubercular Agents / chemical synthesis*
  • Antitubercular Agents / chemistry
  • Antitubercular Agents / pharmacology*
  • Drug Evaluation, Preclinical
  • Imidazoles / chemical synthesis*
  • Imidazoles / chemistry
  • Imidazoles / pharmacology*
  • Microbial Sensitivity Tests
  • Mycobacterium tuberculosis / drug effects

Substances

  • Antitubercular Agents
  • Imidazoles