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

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...

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Bibliographic Details
Published in:Journal of medicinal chemistry 1982-11, Vol.25 (11), p.1358-1363
Main Authors: Kanao, Munefumi, Hashizume, Takeshi, Ichikawa, Yoshifumi, Irie, Kiyoshi, Isoda, Sumiro
Format: Article
Language:English
Subjects:
Animals
Chemical Phenomena
Chemistry
Colon - drug effects
Dogs
Electric Stimulation
Female
Male
Muscle Contraction - drug effects
Muscle, Smooth - drug effects
Naphthalenes - chemical synthesis
Parasympatholytics - chemical synthesis
Stomach - drug effects
Structure-Activity Relationship
Tetrahydronaphthalenes - chemical synthesis
Tetrahydronaphthalenes - pharmacology
Vagus Nerve - physiology
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Summary: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.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm00353a016