Synthesis, Structure and Cytoprotective Activity of New Derivatives of 4-Aryl-3-Aminopyridin-2(1H)-One
Shulgau Z. Palamarchuk I. Dezhko E. Sergazy S. Urazbayeva A. Safarova Y. Gulyayev A. Gatilov Y. Kulakov I.
August 2025Multidisciplinary Digital Publishing Institute (MDPI)
Molecules
2025#30Issue 16
As a continuation of our research on the synthesis and study of biological properties of new derivatives of 3-aminopyridin-2(1H)-ones, we investigated the Leuckart–Wallach and Eschweiler–Clarke reactions with selected 3-aminopyridin-2(1H)-ones and 3-(arylmethyl)pyridin-2(1H)-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(1H)-ones and 3-(arylmethyl)pyridin-2(1H)-ones with an aqueous solution of formaldehyde result in the formation of tertiary N–benzyl(methyl)amino)-pyridin-2(1H)-ones in almost quantitative yield. The 3-aminopyridin-2(1H)-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.
3-(arylmethyl)-6-methyl-4-arylpyridin-2(1H)-ones , 3-aminopyridin-2(1H)-one derivatives , cytoprotective activity , Leuckart-Wallach and Eschweiler-Clarke reactions , X-ray structural analysis
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National Laboratory Astana, Nazarbayev University, Kabanbai Batyr Ave. 53, Astana, Z05H0P9, Kazakhstan
CF “Institute of Innovative and Preventive Medicine”, Alikhan Bokeikhan Street, Building 1, Astana, Z05M0M4, Kazakhstan
Department of Science Development, Astana Medical University, Beibitshilik St 49/A, Astana, Z10K9D9, Kazakhstan
School of Natural Sciences, Tyumen State University, 15a Perekopskaya St., Tyumen, 625003, Russian Federation
N.N. Vorozhtsov Novosibirsk Institute of Organic Chemistry, Siberian Branch of the Russian Academy of Science, 9 Akademika Lavrientieva Ave., Novosibirsk, 630090, Russian Federation
National Laboratory Astana
CF “Institute of Innovative and Preventive Medicine”
Department of Science Development
School of Natural Sciences
N.N. Vorozhtsov Novosibirsk Institute of Organic Chemistry
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