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ID: ALA1136893
Journal: Bioorg Med Chem Lett
Title: Discovery of novel spiro-piperidine derivatives as highly potent and selective melanin-concentrating hormone 1 receptor antagonists.
Authors: Suzuki T, Moriya M, Sakamoto T, Suga T, Kishino H, Takahashi H, Ishikawa M, Nagai K, Imai Y, Sekino E, Ito M, Iwaasa H, Ishihara A, Tokita S, Kanatani A, Sato N, Fukami T.
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 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.
CiteXplore: 19403308