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Identification of 2-aminobenzimidazoles as potent melanin-concentrating hormone 1-receptor (MCH1R) antagonists |
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| 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 |
| Affiliation: | Tsukuba Research Institute, Banyu Pharmaceutical Co., Ltd, Okubo-3, Tsukuba, Ibaraki 300-2611, Japan |
| 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. |
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