Discovery of imidazo[1,2-a]pyridines as potent MCH1R antagonists

被引：18

作者：

Kishino, Hiroyuki ^{[1
]}

Moriya, Minoru ^{[1
]}

Sakuraba, Shunji ^{[1
]}

Sakamoto, Toshihiro ^{[1
]}

Takahashi, Hidekazu ^{[1
]}

Suzuki, Takao ^{[1
]}

Moriya, Ryuichi ^{[1
]}

Ito, Masahiko ^{[1
]}

Iwaasa, Hisashi ^{[1
]}

Takenaga, Norihiro ^{[1
]}

Ishihara, Akane ^{[1
]}

Kanatani, Akio ^{[1
]}

Sato, Nagaaki ^{[1
]}

Fukami, Takehiro ^{[1
]}

机构：

[1] Banyu Pharmaceut Co Ltd, Merck Res Labs, Tsukuba Res Inst, Tsukuba, Ibaraki 3002611, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 16期

关键词：

Melanin-concentrating hormone; MCH1R antagonists; Imidazo[1,2-a]pyridine; Obesity; MELANIN-CONCENTRATING HORMONE; SMALL-MOLECULE ANTAGONISTS; RECEPTOR-1; MCH-R1; HORMONE-RECEPTOR-1; ANTAGONISTS; MICE; OBESITY; SYSTEM;

D O I：

10.1016/j.bmcl.2009.06.101

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of imidazo[1,2-a] pyridine derivatives was identified and evaluated for MCH1R binding and antagonistic activity. Introduction of a methyl substituent at the 3-position of imidazo[1,2-a] pyridine provided compounds with a significant improvement in MCH1R affinity. Representative compounds in this series exhibited good potency and brain exposure in rats. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：4589 / 4593

页数：5

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