title: Discovery of imidazo[1,2-a]pyridines as potent MCH1R antagonists.
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.
authors.affiliation: Tsukuba Research Institute, Merck Research Laboratories, Banyu Pharmaceutical Co, Ltd, Okubo 3, Tsukuba, Ibaraki 300-2611, Japan.
authors.forename: Hiroyuki
authors.initials: H
authors.lastname: Kishino
authors.forename: Minoru
authors.initials: M
authors.lastname: Moriya
authors.forename: Shunji
authors.initials: S
authors.lastname: Sakuraba
authors.forename: Toshihiro
authors.initials: T
authors.lastname: Sakamoto
authors.forename: Hidekazu
authors.initials: H
authors.lastname: Takahashi
authors.forename: Takao
authors.initials: T
authors.lastname: Suzuki
authors.forename: Ryuichi
authors.initials: R
authors.lastname: Moriya
authors.forename: Masahiko
authors.initials: M
authors.lastname: Ito
authors.forename: Hisashi
authors.initials: H
authors.lastname: Iwaasa
authors.forename: Norihiro
authors.initials: N
authors.lastname: Takenaga
authors.forename: Akane
authors.initials: A
authors.lastname: Ishihara
authors.forename: Akio
authors.initials: A
authors.lastname: Kanatani
authors.forename: Nagaaki
authors.initials: N
authors.lastname: Sato
authors.forename: Takehiro
authors.initials: T
authors.lastname: Fukami
mesh_terms: D000818:Animals; D019440:Anti-Obesity Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D016466:CHO Cells; D006224:Cricetinae; D003412:Cricetulus; D055808:Drug Discovery; D006801:Humans; D011725:Pyridines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D051381:Rats; D017481:Receptors, Somatostatin / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D019440:Anti-Obesity Agents; C103263:MCHR1 protein, human; D011725:Pyridines; D017481:Receptors, Somatostatin