Studies on Spasmolytics. III. Synthesis and Anticholinergic Activity 4-Acyloxy-1-(1, 3-dioxolan-2-ylmethyl) piperidines and Their Quaternary Salts

SABURO SUGAI; YOSHIHIRO HASEGAWA; YOSHIO KAJIWARA; SEIICHIRO YOSHIDA; SANYA AKABOSHI

doi:10.1248/cpb.32.1126

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

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Keywords: structure-activity relationship

JOURNAL FREE ACCESS

1984 Volume 32 Issue 3 Pages 1126-1134

DOI https://doi.org/10.1248/cpb.32.1126

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Abstract

Twenty-one derivatives of 4-acyloxy-1-(1, 3-dioxolan-2-ylmethyl) piperidines (2) and their quaternary salts (6) were synthesized and tested for anticholinergic activities. The piperidine derivatives (2) exhibit moderate activities. Among the quaternary salts (6), the trans-isomers were always more active than the corresponding cis-isomers.

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