Synthesis, Structure and Cytoprotective Activity of New Derivatives of 4-Aryl-3-Aminopyridin-2(1)-One.

As a continuation of our research on the synthesis and study of biological properties of new derivatives of 3-aminopyridin-2(1)-ones, we investigated the Leuckart-Wallach and Eschweiler-Clarke reactions with selected 3-aminopyridin-2(1)-ones and 3-(arylmethyl)pyridin-2(1)-ones. It was found that under the conditions of the Leuckart-Wallach reaction with aromatic aldehydes in formic acid, mainly formamides of the indicated 3-aminopyridones are formed. The Eschweiler-Clarke reaction of 3-aminopyridin-2(1)-ones and 3-(arylmethyl)pyridin-2(1)-ones with an aqueous solution of formaldehyde result in the formation of tertiary N-benzyl(methyl)amino)-pyridin-2(1)-ones in almost quantitative yield. The 3-aminopyridin-2(1)-ones derivatives synthesized by us were used for the biological screening of cytoprotective activity in the MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) test to determine the viability of fibroblast cells isolated from the NIH/Swiss mouse embryo (NIH/3T3, Gibco). It was found that many of the studied compounds under the conditions of our experiment exhibited significant cytoprotective effects, thereby enhancing cell survival.