Optimization of (4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepine-5-ylidene)ace tamide derivatives as arginine vasopressin V sub(2) receptor agonists and discussion of their binding modes

A series of (4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepine-5-ylidene)ace tamide derivatives were optimized to achieve potent agonistic activity, both in vitro and in vivo, for the arginine vasopressin V sub(2) receptor, resulting in the eventual discovery of compound 1g. Molecular modeling of com...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry 2009-12, Vol.17 (24), p.8161-8167
Main Authors: Tsukamoto, Issei, Koshio, Hiroyuki, Orita, Masaya, Saitoh, Chikashi, Yanai-Inamura, Hiroko, Kitada-Nozawa, Chika, Yamamoto, Eisaku, Yatsu, Takeyuki, Sakamoto, Shuichi, Tsukamoto, Shin-Ichi
Format: Article
Language:English
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Summary:A series of (4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepine-5-ylidene)ace tamide derivatives were optimized to achieve potent agonistic activity, both in vitro and in vivo, for the arginine vasopressin V sub(2) receptor, resulting in the eventual discovery of compound 1g. Molecular modeling of compound 1g with V sub(2) receptor was also examined to evaluate the binding mode of this series of compounds.
ISSN:0968-0896
DOI:10.1016/j.bmc.2009.10.038