Synthesis and SAR studies of bicyclic amine series GPR119 agonists

被引：24

作者：

Sakairi, Masao ^{[1
]}

Kogami, Masakazu ^{[1
]}

Torii, Masafumi ^{[1
]}

Kataoka, Hiroyo ^{[1
]}

Fujieda, Hiroki ^{[1
]}

Makino, Mitsuhiro ^{[1
]}

Kataoka, Daisuke ^{[1
]}

Okamoto, Ryuji ^{[1
]}

Miyazawa, Toshiyuki ^{[1
]}

Okabe, Morio ^{[1
]}

Inoue, Megumi ^{[1
]}

Takahashi, Naoki ^{[1
]}

Harada, Satoko ^{[1
]}

Watanabe, Nobuhide ^{[1
]}

机构：

[1] Sanwa Kagaku Kenkyusho Co Ltd, Drug Discovery Labs, Inabe, Mie 5110406, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2012年 / 22卷 / 15期

关键词：

GPR119; agonist; Bicyclic amine; Indanone; Basic nitrogen; oGTT; scGTT; PROTEIN-COUPLED RECEPTOR; METABOLIC-DISORDERS; DISCOVERY; POTENT; SECRETION; AGENTS; CELLS;

D O I：

10.1016/j.bmcl.2012.05.117

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

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 oGTT and scGTT in the rodent model. (C) 2012 Elsevier Ltd. All rights reserved.

引用

页码：5123 / 5128

页数：6

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