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Synthesis and neurotropic activity of new 3-(arylmethyl)aminopyridine-2(1H)-one
Chemical Papers ( IF 2.2 ) Pub Date : 2021-05-19 , DOI: 10.1007/s11696-021-01696-7
Irina V. Palamarchuk , Zarina T. Shulgau , Margarita A. Kharitonova , Ivan V. Kulakov

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



中文翻译:

新型 3-(arylmethyl)aminopyridine-2(1H)-one 的合成及亲神经活性

3-氨基-6-甲基-4-苯基吡啶-2(1 H )-one与芳香醛反应生成相应的席夫碱,用硼氢化钠还原生成3-(芳基甲基氨基)-6-甲基-4-苯基吡啶-2(1 H )-ones。所有制备的化合物的结构均通过1 H 和13 C NMR 光谱证明。对体内合成化合物的初步评估是通过“明暗盒测试”的镇静(抗焦虑)活性和 Porsolt 的“行为绝望测试”的抗抑郁活性进行的。3-(芳基甲基氨基)-6-甲基-4-苯基吡啶-2(1 H)-一种比对照药物(美西多和阿米替林)具有更高潜在神经活性的药物被检测到。

图形摘要

更新日期:2021-07-22
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