新型螺哌啶衍生物作为高效且选择性的促黑素细胞激素1受体拮抗剂的发现
Discovery of novel spiro-piperidine derivatives as highly potent and selective melanin-concentrating hormone 1 receptor antagonists.
作者信息
Suzuki Takao, Moriya Minoru, Sakamoto Toshihiro, Suga Takuya, Kishino Hiroyuki, Takahashi Hidekazu, Ishikawa Makoto, Nagai Keita, Imai Yumiko, Sekino Etsuko, Ito Masahiko, Iwaasa Hisashi, Ishihara Akane, Tokita Shigeru, Kanatani Akio, Sato Nagaaki, Fukami Takehiro
机构信息
Department of Medicinal Chemistry, Tsukuba Research Institute, Merck Research Laboratories, Banyu Pharmaceutical Co, Ltd, Tsukuba, Ibaraki, Japan.
出版信息
Bioorg Med Chem Lett. 2009 Jun 1;19(11):3072-7. doi: 10.1016/j.bmcl.2009.04.016. Epub 2009 Apr 9.
Optimization of high-throughput screening hit 1a led to the identification of a novel spiro-piperidine class of melanin-concentrating hormone 1 receptor (MCH-1R) antagonists. Compound 3c was identified as a highly potent and selective MCH-1R antagonist, which has an IC(50) value of 0.09 nM at hMCH-1R. The synthesis and structure-activity relationships of the novel spiro-piperidine MCH-1R antagonists are described.
对高通量筛选命中化合物1a进行优化，从而鉴定出一类新型的螺哌啶类黑色素浓缩激素1受体（MCH-1R）拮抗剂。化合物3c被鉴定为一种高效且具选择性的MCH-1R拮抗剂，其对人MCH-1R的IC(50)值为0.09 nM。本文描述了新型螺哌啶类MCH-1R拮抗剂的合成及其构效关系。
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