ISSN print edition: 0366-6352 ISSN electronic edition: 1336-9075 Registr. No.: MK SR 9/7 Published monthly

Synthesis and Antimycobacterial, Antifungal, and Photosynthesis-Inhibiting Evaluation of Some Anilides of Substituted Pyrazine-2-carboxylic Acids

M. Doležal, R. Vičík, M. Miletín, and K. Kráľová

Department of Pharmaceutical Chemistry and Drug Control, Charles University in Prague, Faculty of Pharmacy in Hradec Králové, CZ-500 05 Hradec Králové

Abstract: Condensation of chlorides of substituted pyrazine-2-carboxylic acids with ring-substituted anilines yielded a series of anilides of 6-chloropyrazine-2-carboxylic, 5-(1,1-dimethylethyl) pyrazine-2-carboxylic or 6-chloro-5- (1,1-dimethylethyl)pyrazine-2-carboxylic acids. Products were tested for their antimycobacterial. antifungal, and photosynthesis-inhibiting activity. Some of them exhibited significative activity against Mycobacterium tuberculosis (inhibition > 50 % at MIC = 12.5 μg cm^-3). The most active compound (88 %) was 6-chloro-5-(1,1-dimethylethyl)pyrazine-2- carboxylic acid 3-fluoroanilide.

Full paper in Portable Document Format: 544a245.pdf

Chemical Papers 54 (4) 245–248 (2000)