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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis and vasodilation activity of some novel bis(3-pyridinecarbonitrile) derivatives.
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Synthesis and vasodilation activity of some novel bis(3-pyridinecarbonitrile) derivatives.

机译：一些新型的双（3-吡啶甲腈）衍生物的合成和血管舒张活性。

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摘要

A variety of bis(2-alkoxy-6-aryl-3-pyridinecarbonitriles) 4a-m were prepared via reaction of bis(2-propen-1-ones) 3a-g with malononitrile in the appropriate alcohol in the presence of KOH. The reaction was assumed to take place via Michael addition followed by cyclization due to the alkoxide nucleophilic attack at one of the nitrile groups. This assumption was substantiated by the reaction of ylidenemalononitrile 5 with the corresponding acetophenone 2 in the appropriate alcohol in the presence of KOH. The starting bis(2-propen-1-ones) 3e and f were prepared stereoselectively as E,E'-geometric isomer via condensation of bisbenzaldehyde 1 with substituted acetophenones 2e and f in ethanolic KOH solution. Vasodilating activity screening of the synthesized compounds 4a-g and 4i-m utilizing isolated rat's thoracic aorta pre-contracted by norepinephrine hydrochloride exhibited that many of the tested compounds reveal considerable vasodilating properties, especially 4e and f which reveal remarkable activities.
机译：通过在适当的醇中，在KOH存在下，使双（2-丙烯-1-酮）3a-g与丙二腈在适当的醇中反应，制备了多种双（2-烷氧基-6-芳基-3-吡啶腈）4a-m。假定该反应通过迈克尔加成发生，然后由于在腈基之一上的醇盐亲核攻击而环化。通过在适当的醇中在KOH存在下使亚甲基丙二腈5与相应的苯乙酮2反应来证实该假设。起始双（2-丙烯-1-酮）3e和f通过双苯甲醛1与取代的苯乙酮2e和f在乙醇KOH溶液中的缩合立体选择性地制备为E，E′-几何异构体。利用去甲肾上腺素盐酸盐预收缩的离体大鼠胸主动脉对合成化合物4a-g和4i-m的血管舒张活性筛选显示，许多受试化合物均显示出显着的血管舒张特性，尤其是4e和f具有显着活性。

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