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 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.
D000818:Animals; D055598:Chemical Phenomena; D002621:Chemistry; D003106:Colon / Q000187:drug effects; D004285:Dogs; D004558:Electric Stimulation; D005260:Female; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects; D009281:Naphthalenes / Q000138:chemical synthesis*; D010276:Parasympatholytics / Q000138:chemical synthesis*; D013270:Stomach / Q000187:drug effects; D013329:Structure-Activity Relationship; D013764:Tetrahydronaphthalenes / Q000138:chemical synthesis* / Q000494:pharmacology; D014630:Vagus Nerve / Q000502:physiology
D009281:Naphthalenes; D010276:Parasympatholytics; D013764:Tetrahydronaphthalenes