Nonpeptide angiotensin II receptor antagonists: synthesis, biological activities, and structure-activity relationships of imidazole-5-carboxylic acids bearing alkyl, alkenyl …

H Yanagisawa, Y Amemiya, T Kanazaki…

Index: Yanagisawa, Hiroaki; Amemiya, Yoshiya; Kanazaki, Takuro; Shimoji, Yasuo; Fujimoto, Koichi; Kitahara, Yoshiko; Sada, Toshio; Mizuno, Makoto; Ikeda, Masahiro; Miyamoto, Shuichi; Furukawa, Youji; Koike, Hiroyuki Journal of Medicinal Chemistry, 1996 , vol. 39, # 1 p. 323 - 338

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Citation Number: 142

Abstract

A series of imidazole-5-carboxylic acids bearing alkyl, alkenyl, and hydroxyalkyl substituents at the 4-position and their related compounds were prepared and evaluated for their antagonistic activities to the angiotensin II (AII) receptor. Among them, the 4-(1-hydroxyalkyl) imidazole derivatives had strong binding affinity to the AII receptor and potently inhibited the AII-induced pressor response by intravenous administration. Various esters of these acids ...