870862-12-7Relevant articles and documents
Discovery of novel spiro-piperidine derivatives as highly potent and selective melanin-concentrating hormone 1 receptor antagonists
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
scheme or table, p. 3072 - 3077 (2010/02/28)
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.
