| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1372240 | Bioorganic & Medicinal Chemistry Letters | 2009 | 5 Pages |
Abstract
A series of 2-aminobenzimidazole-based MCH1R antagonists was identified by core replacement of the aminoquinoline lead 1. Subsequent modification of the 2- and 5-positions led to improvement in potency and intrinsic clearance. Compound 25 exhibited good plasma and brain exposure, and attenuated MCH induced food intake at 30 mg/kg PO in rats.
Graphical abstractWe report the identification of potent and brain-penetrable 2-aminobenzimidazole based MCH1R antagonist 25.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Minoru Moriya, Hiroyuki Kishino, Shunji Sakuraba, Toshihiro Sakamoto, Takuya Suga, Hidekazu Takahashi, Takao Suzuki, Masahiko Ito, Junko Ito, Ryuichi Moriya, Norihiro Takenaga, Hisashi Iwaasa, Akane Ishihara, Akio Kanatani, Takehiro Fukami,