Nonpeptide arginine vasopressin antagonists for both V1A and V2 receptors: synthesis and pharmacological properties of 2-phenyl-4'-(2, 3, 4, 5-tetrahydro-1H-1, 5- …

…, H Koshio, K Sakamoto, N TANIGUCHI…

Index: Matsuhisa, Akira; Koshio, Hiroyuki; Sakamoto, Kenichiro; Taniguchi, Nobuaki; Yatsu, Takeyuki; Tanaka, Akihiro Chemical and Pharmaceutical Bulletin, 1998 , vol. 46, # 10 p. 1566 - 1579

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Citation Number: 30

Abstract

A series of compounds structurally related to 2-phenyl-4'-(2, 3, 4, 5-tetrahydro-1H-1, 5- benzodiazepine-1-carbonyl) benzanilide was synthesized and demonstrated to have arginine vasopressin (AVP) antagonist activity for both V 1A and V 2 receptors. The introduction of a hydrophilic substituent group into the 5-position of the benzodiazepine ring resulted in an increase in oral availability. Especially, the (3-pyridyl) methyl (31b), the 2-(4- ...