Discovery of imidazo[1,2-a]pyridines as potent MCH1R antagonists |
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| Authors: | Hiroyuki Kishino Minoru Moriya Shunji Sakuraba Toshihiro Sakamoto Hidekazu Takahashi Takao Suzuki Ryuichi Moriya Masahiko Ito Hisashi Iwaasa Norihiro Takenaga Akane Ishihara Akio Kanatani Nagaaki Sato Takehiro Fukami |
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| Affiliation: | Tsukuba Research Institute, Merck Research Laboratories, Banyu Pharmaceutical Co., Ltd, Okubo 3, Tsukuba, Ibaraki 300-2611, Japan |
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| 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. |
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