Synthesis and SAR studies of bicyclic amine series GPR119 agonists

…, M Inoue, N Takahashi, S Harada, N Watanabe

文献索引：Sakairi, Masao; Kogami, Masakazu; Torii, Masafumi; Kataoka, Hiroyo; Fujieda, Hiroki; Makino, Mitsuhiro; Kataoka, Daisuke; Okamoto, Ryuji; Miyazawa, Toshiyuki; Okabe, Morio; Inoue, Megumi; Takahashi, Naoki; Harada, Satoko; Watanabe, Nobuhide Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 15 p. 5123 - 5128

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被引用次数: 15

摘要

We disclosed a novel series of G-protein coupled receptor 119 (GPR119) agonists based on a bicyclic amine scaffold. Through the optimization of hit compound 1, we discovered that the basic nitrogen atom of bicyclic amine played an important role in GPR119 agonist activity expression and that an indanone in various bicyclic rings was suitable in this series of compounds. The indanone derivative 2 showed the effect of plasma glucose control in ...