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取代(ω-氨基烷氧基)苯衍生物的合成及抗抑郁活性

Synthesis and antidepressant activity of substituted (omega-aminoalkoxy)benzene derivatives.

作者信息

Kikumoto R, Tobe A, Tonomura S

出版信息

J Med Chem. 1981 Feb;24(2):145-8. doi: 10.1021/jm00134a004.

Abstract

A series of substituted (omega-aminoalkoxy)benzene derivatives has been synthesized and screened for potential antidepressant activities. The effect of structural variation of these molecules has been systematically examined. Antidepressant activity was clearly displayed by 2-benzyl-1-[4-(methylamino)butoxy]benzene (7), 2-(2-hydroxybenzyl)-1-[4-(methylamino)butoxy]benzene (19), 1-[4-(methylamino)butoxy]-2-phenoxybenzene (29), and 1-[4-(methylamino)butoxy]-2-(phenylthio)benzene (31) in further pharmacological studies. These compounds did not possess the anticholinergic, antihistaminic, and muscle-relaxant side effects common to tricyclic antidepressants.

摘要

已经合成了一系列取代的(ω-氨基烷氧基)苯衍生物,并对其潜在的抗抑郁活性进行了筛选。系统地研究了这些分子结构变化的影响。在进一步的药理研究中,2-苄基-1-[4-(甲氨基)丁氧基]苯(7)、2-(2-羟基苄基)-1-[4-(甲氨基)丁氧基]苯(19)、1-[4-(甲氨基)丁氧基]-2-苯氧基苯(29)和1-[4-(甲氨基)丁氧基]-2-(苯硫基)苯(31)显示出明显的抗抑郁活性。这些化合物不具有三环类抗抑郁药常见的抗胆碱能、抗组胺和肌肉松弛副作用。

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