1266775-27-2Relevant academic research and scientific papers
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)
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.
