Antimycobacterial Evaluation of Pyrazinoic Acid Reversible Derivatives

Title: Antimycobacterial Evaluation of Pyrazinoic Acid Reversible Derivatives

Volume: 17 Issue: 32

Author(s): Martin Dolezal, Diana Kesetovic and Jan Zitko

Affiliation:

Keywords: Pyrazines, in vitro antimycobacterial evaluation, structure-activity relationships, Tuberculosis, pyridine, esters, amide prodrugs, MIC (Minimal Inhibitory Concentration), Lawesson's reagent, Homolytic aroylation

Abstract: Design, results of in vitro antimycobacterial evaluation, and study of structure-activity relationships of various pyrazinecarboxylic acid reversible derivatives are presented. This review deals with some pyrazinamide analogues/prodrugs derived from Nphenylpyrazine- 2-carboxamides (1), arylaminopyrazine-2,5-dicarbonitriles (2), aryl/alkylsulphanylpyrazines (3,4), and aroylpyrazines (5) effecting > 50% inhibition in the primary antimycobacterial screen. The promising pyrazine candidates for further antimycobacterial evaluation were discovered. Results give good view onto structure-activity relationships of these analogues and promise even better activity of new compounds prepared after some structure optimization experiments.

Cite this article as:

Dolezal Martin, Kesetovic Diana and Zitko Jan, Antimycobacterial Evaluation of Pyrazinoic Acid Reversible Derivatives, Current Pharmaceutical Design 2011; 17 (32) . https://dx.doi.org/10.2174/138161211798194477