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Synthesis, antimycobacterial and antifungal evaluation of 3-arylaminopyrazine-2,5-dicarbonitriles
L Palek, J Dvorak, M Svobodova, V Buchta, J Jampilek, M Dolezal
Archiv der Pharmazie.
2008 ;
341 (1) :
61-65.
Language English Country Germany
Persistent link
https://www.medvik.cz/link/bmc10029866
- MeSH
- Absidia drug effects MeSH
- Antifungal Agents pharmacology chemical synthesis MeSH
- Antitubercular Agents pharmacology chemical synthesis MeSH
- Aspergillus fumigatus drug effects MeSH
- Candida drug effects MeSH
- Financing, Organized MeSH
- Microbial Sensitivity Tests MeSH
- Mycobacterium drug effects MeSH
- Nitriles pharmacology chemical synthesis MeSH
- Pyrazinamide analogs & derivatives pharmacology chemical synthesis MeSH
- Pyrazines pharmacology chemical synthesis MeSH
- Trichosporon drug effects MeSH
- Chromatography, High Pressure Liquid MeSH
- Structure-Activity Relationship 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.
References provided by Crossref.org
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- $a Department of Medicinal Chemistry and Drug Control, Charles University Prague, Faculty of Pharmacy in Hradec Kralove, Hradec Kralove, Czech Republic.
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- $a 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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