Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1371980 | Bioorganic & Medicinal Chemistry Letters | 2009 | 7 Pages |
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.
Graphical abstractThe identification of selective and orally active MCH-1R antagonist 4b is reported.Figure optionsDownload full-size imageDownload as PowerPoint slide
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Takao Suzuki, Minoru Kameda, Makoto Ando, Hiroshi Miyazoe, Etsuko Sekino, Satoru Ito, Kouta Masutani, Kaori Kamijo, Akihiro Takezawa, Minoru Moriya, Masahiko Ito, Junko Ito, Kazuho Nakase, Hiroko Matsushita, Akane Ishihara, Norihiro Takenaga,