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Substituted Pyrazinecarboxamides: Preparation and Biological Activity
* 1 , 1 , 1 , 2 , 3 , 4
1  Department of Pharmaceutical Chemistry and Drug Control, Faculty of Pharmacy, Charles University, Heyrovskeho 1203, 500 05 Hradec Kralove, Czech Republic
2  Department of Inorganic and Organic Chemistry, Faculty of Pharmacy, Charles University, Heyrovskeho 1203, 500 05 Hradec Kralove, Czech Republic
3  Department of Biological and Medical Sciences, Faculty of Pharmacy, Charles University, Heyrovskeho 1203, 500 05 Hradec Kralove, Czech Republic
4  Institute of Chemistry, Faculty of Natural Sciences, Comenius University, Mlynska Dolina CH-2, 842 15 Bratislava, Slovak Republic

Abstract: Newly synthesised pyrazinamide analogues with carboxamide moiety as a bridging ligands between basic and aromatic areas of molecule were tested for their antifungal and photosynthesis-inhibiting activity. The synthetic approach, analytical and spectroscopic data of all newly synthesized compounds are presented. The highest antifungal effect (MIC < 62.5 µmol l-1) against Candida albicans, the most susceptible fungal strain tested, was found for 6-chloropyrazine-2-carboxylic acid (3-chlorophenyl)amide. The most active inhibitor of oxygen evolution rate in spinach chloroplasts was 5-tert-butyl-6-chloropyrazine-2-carboxylic acid (3-chlorophenyl)amide (IC50 = 47.0 µmol dm-3).
Keywords: substituted amides of pyrazin-2-carboxylic acid; antifungal evaluation; photosynthesis inhibition; spinach chloroplasts

 
 
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