Synthesis and neurotropic activity of new 3-(arylmethyl)aminopyridine-2(1H)-one
Palamarchuk I.V. Shulgau Z.T. Kharitonova M.A. Kulakov I.V.
September 2021Springer Science and Business Media Deutschland GmbH
Chemical Papers
2021#75Issue 94729 - 4739 pp.
The reaction of 3-amino-6-methyl-4-phenylpyridine-2(1H)-one with aromatic aldehydes resulted in the corresponding Schiff bases, which reduction with sodium borohydride led to the formation of 3-(arylmethylamino)-6-methyl-4-phenylpyridine-2(1H)-ones. The structure of all prepared compounds was proved by 1H and 13C NMR spectroscopy. The initial evaluation of the synthesized compounds in vivo was carried out for a tranquilizing (anxiolytic) activity by «light–dark box test» and antidepressant activity by Porsolt’s «behavioral despair test». Several derivatives of 3-(arylmethylamino)-6-methyl-4-phenylpyridine-2(1H)-one with higher potential neurotropic activity than that of the comparator drugs (Mexidol and Amitriptyline) were detected. Graphic abstract: [Figure not available: see fulltext.]
3-(arylmethyl)-6-methyl-4-phenylpyridine-2(1H)-one , 3-amino-6-methyl-4-phenylpyridin-2(1H)-one , Anxiolytic and antidepressant activities
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Institute of Chemistry, Tyumen State University, 15a Perekopskaya St., Tyumen, 625003, Russian Federation
RSE “National Center for Biotechnology” of the Ministry of Education and Science, 13/5 Kurgalzhynskoe road, Nur-Sultan, 010000, Kazakhstan
Institute of Chemistry
RSE “National Center for Biotechnology” of the Ministry of Education and Science
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