S 98 Synthesis, analgesic and antipyretic activity of 2-(antipyrin-4-yl)hydrazones of 1,2,3-triketones and their derivatives [Electronic resource] / E. V. Shchegol'kov, O. G. Khudina, L. V. Anikina, Ya. V. Burgart, V. I. Saloutin // Pharmaceutical Chemistry Journal. - 2006. - Vol. 40, № 7. - P373-376. - Библиогр. : с. 376 (10 назв.) Рубрики: ХИМИЧЕСКИЕ НАУКИ Аннотация: 1,2,3-Triketone 2-(antipyrin-4-yl)hydrazones were synthesized via the azo-coupling reactions of 1,3-diketones with 2-(antipyrin-4-yl)diazonium chloride. The fluoroalkyl-containing hetarylhydrazone enters into cyclocondensation with hydrazines at the 1,3-dicarbonyl fragment to yield 3-tetrafluoroethyl derivatives of pyrazole. It was found that 1,2,3-triketone 2-(antipyrin-4-yl)hydrazones and N-(2-hydroxyethyl)-substituted pyrazole exhibit analgesic activity comparable with that of their structural analog analgin (metamizole sodium), but do not possess antipyretic properties. In contrast, N-phenyl-substituted pyrazole did not exhibit analgesic properties but produced a certain antipyretic effect four hours after pyrogenic administration. Fluoroalkyl-containing compounds are less toxic substances than nonfluorinated 2-(antipyrin-4-yl)hydrazone and analgin. \\\\Expert2\\nbo\\Pharmaceutical Chemistry Journal\\2006, 40 (7), 373-376.pdf |