Chemical and Pharmaceutical Bulletin p. 1566 - 1579 (1998)
Update date:2022-08-05
Matsuhisa, Akira
Koshio, Hiroyuki
Sakamoto, Kenichiro
Taniguchi, Nobuaki
Yatsu, Takeyuki
Tanaka, Akihiro
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 V2 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- methyl)-1,4-diazepan-1-yl)-2-oxoethyl (32i), and the 2-(4-methylpiperazin-1- yl)ethyl (33g) derivatives exhibited high antagonist activities and high oral availability. Details of the synthesis and pharmacological properties of this series are presented.
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