Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1373751 | Bioorganic & Medicinal Chemistry Letters | 2009 | 6 Pages |
Abstract
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 IC50 value of 0.09 nM at hMCH-1R. The synthesis and structure–activity relationships of the novel spiro-piperidine MCH-1R antagonists are described.
Graphical abstractThe identification of highly potent and selective MCH-1R antagonist 3c is reported.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Takao Suzuki, Minoru Moriya, Toshihiro Sakamoto, Takuya Suga, Hiroyuki Kishino, Hidekazu Takahashi, Makoto Ishikawa, Keita Nagai, Yumiko Imai, Etsuko Sekino, Masahiko Ito, Hisashi Iwaasa, Akane Ishihara, Shigeru Tokita, Akio Kanatani, Nagaaki Sato,