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Synthesis, Antimycobacterial and Antifungal Evaluation of 3‐Arylaminopyrazine‐2,5‐dicarbonitriles
Author(s) -
Palek Lukáš,
Dvořák Jaroslav,
Svobodová Michaela,
Buchta Vladimír,
Jampílek Josef,
Doležal Martin
Publication year - 2008
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.200700119
Subject(s) - antimycobacterial , pyrazinamide , mycobacterium tuberculosis , chemistry , pyrazine , stereochemistry , mycobacterium , in vitro , biological activity , combinatorial chemistry , tuberculosis , biochemistry , medicine , pathology
This paper describes preparation and biological evaluation of pyrazinamide analogues. Pyrazinamide with its simple structure gives a good opportunity for further modification regarding an increase of its antimycobacterial activity. We prepared a series of compounds derived from pyrazine‐2,5‐dicarbonitrile with arylamino substitution in position 3. All compounds were assayed in vitro against major Mycobacterium and various Fungi species. The best activity was found in 3‐{[3‐(trifluoromethyl)phenyl]amino}pyrazine‐2,5‐dicarbonitrile 11 with the value of 6.25 μmol –1 against M. tuberculosis H 37 Rv and moderate activity against minor Mycobacterium pathogens.