Journal of Medicinal Chemistry 1982-11-01

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

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

文献索引：J. Med. Chem. 25(!1) , 1358-1363, (1982)

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摘要

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.