Abstract
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.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Absidia / drug effects
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Antifungal Agents / chemical synthesis*
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Antifungal Agents / pharmacology
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Antitubercular Agents / chemical synthesis*
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Antitubercular Agents / pharmacology
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Aspergillus fumigatus / drug effects
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Candida / drug effects
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Chromatography, High Pressure Liquid
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Microbial Sensitivity Tests
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Mycobacterium / drug effects
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Nitriles / chemical synthesis*
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Nitriles / pharmacology
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Pyrazinamide / analogs & derivatives*
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Pyrazinamide / chemical synthesis*
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Pyrazinamide / pharmacology
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Pyrazines / chemical synthesis*
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Pyrazines / pharmacology
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Structure-Activity Relationship
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Trichosporon / drug effects
Substances
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3-((3-(trifluoromethyl)phenyl)amino)pyrazine-2,5-dicarbonitrile
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Antifungal Agents
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Antitubercular Agents
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Nitriles
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Pyrazines
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Pyrazinamide