鎮痙薬の研究(第4報)N-(2-Acyloxyethyl)-N-(1,3-dioxolan-2-and 4-ylmethyl)-N, N-dimethylammonium誘導体の合成と抗アセチルコリン作用

菅井 三郎; 長谷川 賀洋; 梶原 良夫; 内藤 泰男; 吉田 誠一郎; 赤星 三彌

doi:10.1248/yakushi1947.103.10_1034

Studies on Spasmolytics. IV. Synthesis and Anticholinergic Activity of N-(2-Acyloxyethyl)-N-(1, 3-dioxolan-2-and 4-ylmethyl)-N, N-dimethylammonium Derivatives

SABURO SUGAI, YOSHIHIRO HASEGAWA, YOSHIO KAJIWARA, YASUO NAITO, SEIICHIRO YOSHIDA, SANYA AKABOSHI

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Keywords: synthesis, N-(2-acyloxyethyl)-N-(1, 3-dioxolan-2- and 4-ylmethyl)-N-methylamine derivative, quaternization, N-(2-acyloxyethyl)-N, N-dimethyl-N-(1, 3-dioxolan-2-and 4-ylmethyl) ammonium derivative, anticholinergic activity, structure-activity relationship

JOURNAL FREE ACCESS

1983 Volume 103 Issue 10 Pages 1034-1041

DOI https://doi.org/10.1248/yakushi1947.103.10_1034

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Abstract

N-(2-Acyloxyethyl)-N, N-dimethyl-N-(1, 3-dioxolan-2-and 4-ylmethyl) ammonium compounds were synthesized and tested for anticholinergic activity. It was found that among these compounds the N-(2-acyloxyethyl)-N-(1, 3-dioxolan-2-ylmethyl) ammonium derivatives exhibited more potent activities than the N-(2-acyloxyethyl)-N-(1, 3-dioxolan-4-ylmethyl) ammonium and N-(3-acyloxypropyl)-N-(1, 3-dioxolan-4-ylmethyl) ammonium ones.

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