1192035-81-6Relevant articles and documents
Discovery of novel diarylketoxime derivatives as selective and orally active melanin-concentrating hormone 1 receptor antagonists
Suzuki, Takao,Kameda, Minoru,Ando, Makoto,Miyazoe, Hiroshi,Sekino, Etsuko,Ito, Satoru,Masutani, Kouta,Kamijo, Kaori,Takezawa, Akihiro,Moriya, Minoru,Ito, Masahiko,Ito, Junko,Nakase, Kazuho,Matsushita, Hiroko,Ishihara, Akane,Takenaga, Norihiro,Tokita, Shigeru,Kanatani, Akio,Sato, Nagaaki,Fukami, Takehiro
scheme or table, p. 5339 - 5345 (2010/06/16)
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.
