Synthesis and pharmacological evaluation of 1-oxo-2-(3-piperidyl)-1, 2, 3, 4-tetrahydroisoquinolines and related analogues as a new class of specific bradycardic …

…, A Kakefuda, T Watanabe, N Ishii, K Wada…

Index: Kubota, Hideki; Kakefuda, Akio; Watanabe, Toshihiro; Ishii, Noe; Wada, Koichi; Masuda, Noriyuki; Sakamoto, Shuichi; Tsukamoto, Shin-ichi Journal of Medicinal Chemistry, 2003 , vol. 46, # 22 p. 4728 - 4740

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Citation Number: 15

Abstract

A series of 1-oxo-2-(3-piperidyl)-1, 2, 3, 4-tetrahydroisoquinolines and related analogues were prepared and evaluated for their bradycardic activities in isolated right atrium and in anesthetized rats.(±)-6, 7-Dimethoxy-2-{1-[3-(3, 4-methylenedioxyphenoxy) propyl]-3- piperidyl}-1, 2, 3, 4-tetrahydroisoquinoline (4) was chosen as a lead, and structural modifications were performed on the tetrahydroisoquinoline ring and the terminal aromatic ...