Collect. Czech. Chem. Commun.
1995, 60, 1236-1241
https://doi.org/10.1135/cccc19951236
Synthesis and Antituberculotic Activity of Some Substituted 3-Arylamino-5-cyano-2-pyrazinecarboxamides
Martin Doležala, Jiří Hartla, Antonín Lyčkab, Vladimír Buchtac and Želmíra Odlerovád
a Department of Medicinal Chemistry and Drug Control, Faculty of Pharmacy, Charles University, 500 05 Hradec Králové, Czech Republic
b Research Institute of Organic Syntheses, 532 18 Pardubice-Rybitví, Czech Republic
c Department of Biological and Medicinal Sciences, Faculty of Pharmacy, Charles University, 500 05 Hradec Králové, Czech Republic
d Institute of Preventive and Clinic Medicine, 833 01 Bratislava, Slovak Republic
Abstract
Nucleophilic substitution of 3-chloro-5-cyano-2-pyrazinecarboxamide by substituted anilines afforded substituted 3-arylamino-5-cyano-2-pyrazinecarboxamides I-X. The structures of compounds were confirmed by elemental analysis, UV, IR and 1H NMR spectra. The assessment of in vitro antimycotic and antimycobacterial activities of the compounds was carried out. The highest antituberculotic activity against M. tuberculosis in this series was shown by 3-anilino- 5-cyano-2-pyrazinecarboxamide (I), whose efficacy was the same as that of pyrazinecarboxamide.
