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3-氮杂双环[3.2.2]壬烷衍生物的合成及镇咳活性

Synthesis and antitussive activity of 3-azabicyclo[3.2.2]nonane derivatives.

作者信息

Arya V P, Kaul C L, Grewal R S

出版信息

Arzneimittelforschung. 1977;27(9):1648-52. doi: 10.1002/chin.197751285.

DOI:10.1002/chin.197751285
PMID:579131
Abstract

Mannich bases derived from a number of substituted acetophenones and propiophenones and 3-azabicyclo[3.2.2]nonane have been evaluated for antitussive activity. One of these compounds was as potent as codeine and dextromethorphan in its antitussive activity. The most potent compound of the series, 3-(3-azabicyclo[2.2.2]nonan-3-yl)-4'-benzyloxy-2-methyl propiophenone, also exhibited antimorphine activity. There was no direct correlation between the antitussive effect and antimorphine activity.

摘要

对源自多种取代苯乙酮和苯丙酮以及3-氮杂双环[3.2.2]壬烷的曼尼希碱进行了镇咳活性评估。其中一种化合物的镇咳活性与可待因和右美沙芬相当。该系列中最有效的化合物3-(3-氮杂双环[2.2.2]壬烷-3-基)-4'-苄氧基-2-甲基苯丙酮也表现出抗吗啡活性。镇咳作用和抗吗啡活性之间没有直接相关性。

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