Kishino Hiroyuki, Moriya Minoru, Sakuraba Shunji, Sakamoto Toshihiro, Takahashi Hidekazu, Suzuki Takao, Moriya Ryuichi, Ito Masahiko, Iwaasa Hisashi, Takenaga Norihiro, Ishihara Akane, Kanatani Akio, Sato Nagaaki, Fukami Takehiro
Tsukuba Research Institute, Merck Research Laboratories, Banyu Pharmaceutical Co, Ltd, Okubo 3, Tsukuba, Ibaraki 300-2611, Japan.
Bioorg Med Chem Lett. 2009 Aug 15;19(16):4589-93. doi: 10.1016/j.bmcl.2009.06.101. Epub 2009 Jul 4.
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.
一系列咪唑并[1,2 - a]吡啶衍生物被鉴定并评估其对MCH1R的结合和拮抗活性。在咪唑并[1,2 - a]吡啶的3位引入甲基取代基，使化合物的MCH1R亲和力有显著提高。该系列中的代表性化合物在大鼠中表现出良好的活性和脑内暴露水平。
