Antimycobacterial Evaluation of Pyrazinoic Acid Reversible Derivatives

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

Journal Name: Current Pharmaceutical Design

Volume 17 , Issue 32 , 2011

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

Rights & PermissionsPrintExport Cite as

Article Details

VOLUME: 17
ISSUE: 32
Year: 2011
Page: [3506 - 3514]
Pages: 9
DOI: 10.2174/138161211798194477
Price: $58

Article Metrics

PDF: 6