Discovery of imidazo[1,2-a

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• 作者：Hiroyuki Kishino ; Minoru Moriya ; Shunji Sakuraba ; Toshihiro Sakamoto ; Hidekazu Takahashi ; Takao Suzuki ; Ryuichi Moriya ; Masahiko Ito ; Hisashi Iwaasa ; Norihiro Takenaga ; Akane Ishihara ; Akio Kanatani
• 关键词：Melanin-concentrating hormone ; MCH1R antagonists ; Imidazo[1 ; 2-a]pyridine ; Obesity
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2009
• 出版时间：15 August 2009
• 年：2009
• 卷：19
• 期：16
• 页码：4589-4593
• 全文大小：681 K

文摘

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.