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

…, H Iwaasa, N Takenaga, A Ishihara, A Kanatani…

Index: Kishino, Hiroyuki; Moriya, Minoru; Sakuraba, Shunji; Sakamoto, Toshihiro; Takahashi, Hidekazu; Suzuki, Takao; Moriya, Ryuichi; Ito, Masahiko; Iwaasa, Hisashi; Takenaga, Norihiro; Ishihara, Akane; Kanatani, Akio; Sato, Nagaaki; Fukami, Takehiro Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 16 p. 4589 - 4593

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Citation Number: 10

Abstract

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.