Aminopyrazinoic acid esters as potential antimycobacterial drugs

Ceska Slov Farm. 2013 Apr;62(2):84-8.

Abstract

A series of esters of the 3-aminopyrazine-2-carboxylic acid as potential antimycobacterial drugs was synthesized. A CEM Discover microwave reactor with an autosampler Explorer 24 which served to accelerate the reaction was used for synthesis. The prepared products were characterized by IR, 1H NMR, 13C NMR spectra, elementary analysis and melting points. Log P and ClogP values were calculated. Final products were evaluated in vitro for their antimycobacterial activity. The most active compound was hexyl 3-aminopyrazine-2-carboxylate (7), whose antimycobacterial activity (MIC) against M. tuberculosis H37Rv was 6.25 μg/mL.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antitubercular Agents / chemical synthesis
  • Antitubercular Agents / pharmacology*
  • Esters
  • Microbial Sensitivity Tests
  • Mycobacterium tuberculosis / drug effects*
  • Mycobacterium tuberculosis / growth & development
  • Pyrazines / chemical synthesis
  • Pyrazines / pharmacology*

Substances

  • Antitubercular Agents
  • Esters
  • Pyrazines
  • 3-aminopyrazine-2-carboxylic acid