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解痉剂。2. 1,2,3,4-四氢-2-萘胺衍生物。

Spasmolytic agents. 2. 1,2,3,4-Tetrahydro-2-naphthylamine derivatives.

作者信息

Kanao M, Hashizume T, Ichikawa Y, Irie K, Isoda S

出版信息

J Med Chem. 1982 Nov;25(11):1358-63. doi: 10.1021/jm00353a016.

Abstract

N-[(Benzoyloxy)alkyl]-1,2,3,4-tetrahydro-2-naphthylamine derivatives were synthesized from 1,2,3,4-tetrahydro-2-naphthylamines and evaluated for their spasmolytic. Some of these compounds showed a nerve-selective effect on colon rather than stomach in anesthetized dogs and were found to be equal to or more active than the reference drug (mebeverine). The biological data have indicated some structure-activity relationships. Among these compounds, N-ethyl-N-[6-(3,4-dimethoxybenzoyl)oxy]hexyl]-1,2,3,4-tetrahydro-6-methoxy-2- napththylamine hydrochloride (63) was found to be the most active spasmolytic agent.

摘要

N-[(苯甲酰氧基)烷基]-1,2,3,4-四氢-2-萘胺衍生物由1,2,3,4-四氢-2-萘胺合成,并对其解痉作用进行了评估。在麻醉犬中,其中一些化合物对结肠而非胃表现出神经选择性作用,且发现其活性与参比药物(美贝维林)相当或更高。生物学数据表明了一些构效关系。在这些化合物中,N-乙基-N-[6-(3,4-二甲氧基苯甲酰基)氧基]己基]-1,2,3,4-四氢-6-甲氧基-2-萘胺盐酸盐(63)被发现是活性最高的解痉剂。

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