Synthesis and structure–activity relationships of amide derivatives of (4, 4-difluoro-1, 2, 3, 4-tetrahydro-5H-1-benzazepin-5-ylidene) acetic acid as selective arginine …

…, C Saitoh, H Yanai-Inamura, C Kitada-Nozawa…

文献索引：Tsukamoto, Issei; Koshio, Hiroyuki; Kuramochi, Takahiro; Saitoh, Chikashi; Yanai-Inamura, Hiroko; Kitada-Nozawa, Chika; Yamamoto, Eisaku; Yatsu, Takeyuki; Shimada, Yoshiaki; Sakamoto, Shuichi; Tsukamoto, Shin-ichi Bioorganic and Medicinal Chemistry, 2009 , vol. 17, # 8 p. 3130 - 3141

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被引用次数: 10

摘要

A series of (4, 4-difluoro-1, 2, 3, 4-tetrahydro-5H-1-benzazepin-5-ylidene) acetamide derivatives was synthesized, and their structure–activity relationships were examined in order to identify potent and selective arginine vasopressin V2 receptor agonists. Attempts to substitute other chemical groups in place of the 2-pyridilmethyl moiety of 1a led to the discovery that potent V2 binding affinity could be obtained with a wide range of functional ...