864756-35-4Relevant articles and documents
Discovery of novel phenylpyridone derivatives as potent and selective MCH1R antagonists
Haga, Yuji,Mizutani, Sayaka,Naya, Akira,Kishino, Hiroyuki,Iwaasa, Hisashi,Ito, Masahiko,Ito, Junko,Moriya, Minoru,Sato, Nagaaki,Takenaga, Norihiro,Ishihara, Akane,Tokita, Shigeru,Kanatani, Akio,Ohtake, Norikazu
, p. 883 - 893 (2011/03/19)
The design, synthesis and structure-activity relationships of a novel class of N-phenylpyridone MCH1R antagonists are described. The core part of the N-phenylpyridone structure was newly designed and the side chain moieties that were attached to the core part were extensively explored. As a result of optimization of the N-phenylpyridone leads, we successfully developed the orally available, and brain-penetrable MCH1R selective antagonist 7c, exhibiting excellent anti-obese effect in diet-induced obese (DIO) mice.