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ID: ALA1155989
Journal: Bioorg Med Chem Lett
Title: Discovery of novel diarylketoxime derivatives as selective and orally active melanin-concentrating hormone 1 receptor antagonists.
Authors: Suzuki T, Kameda M, Ando M, Miyazoe H, Sekino E, Ito S, Masutani K, Kamijo K, Takezawa A, Moriya M, Ito M, Ito J, Nakase K, Matsushita H, Ishihara A, Takenaga N, Tokita S, Kanatani A, Sato N, Fukami T.
Abstract: Optimization of the lead 2a led to the identification of a novel diarylketoxime class of melanin-concentrating hormone 1 receptor (MCH-1R) antagonists. Our focus was directed toward improvement of hERG activity and metabolic stability. The representative derivative 4b showed potent and dose-dependent body weight reduction in diet-induced obese (DIO) C57BL/6J mice after oral administration. The synthesis and structure-activity relationships of the novel diarylketoxime MCH-1R antagonists are described.
CiteXplore: 19683441