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Current Pharmaceutical Design

Editor-in-Chief

ISSN (Print): 1381-6128
ISSN (Online): 1873-4286

Antimycobacterial Evaluation of Pyrazinoic Acid Reversible Derivatives

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

Volume 17, Issue 32, 2011

Page: [3506 - 3514] Pages: 9

DOI: 10.2174/138161211798194477

Price: $65

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.

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


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