Synthesis, antimycobacterial and antifungal evaluation of 3-arylaminopyrazine-2,5-dicarbonitriles
Language English Country Germany Media print
Document type Journal Article, Research Support, Non-U.S. Gov't
- MeSH
- Absidia drug effects MeSH
- Antifungal Agents chemical synthesis pharmacology MeSH
- Antitubercular Agents chemical synthesis pharmacology MeSH
- Aspergillus fumigatus drug effects MeSH
- Candida drug effects MeSH
- Microbial Sensitivity Tests MeSH
- Mycobacterium drug effects MeSH
- Nitriles chemical synthesis pharmacology MeSH
- Pyrazinamide analogs & derivatives chemical synthesis pharmacology MeSH
- Pyrazines chemical synthesis pharmacology MeSH
- Trichosporon drug effects MeSH
- Chromatography, High Pressure Liquid MeSH
- Structure-Activity Relationship MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
- Names of Substances
- 3-((3-(trifluoromethyl)phenyl)amino)pyrazine-2,5-dicarbonitrile MeSH Browser
- Antifungal Agents MeSH
- Antitubercular Agents MeSH
- Nitriles MeSH
- Pyrazinamide MeSH
- Pyrazines MeSH
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 micromol(-1) against M. tuberculosis H(37)Rv and moderate activity against minor Mycobacterium pathogens.
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