927892-36-2Relevant 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
experimental part, 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.
PHENYLPYRIDONE DERIVATIVE
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Page/Page column 29, (2008/12/05)
A compound represented by the formula (I) is contained as an active ingredient: wherein R1 and R2 independently represent a hydrogen atom, a lower alkyl group or the like, or R1 together with a nitrogen atom to which L, Z2 and R1 are attached may form an aliphatic nitrogenated heterocyclic group and R1 and R2 together with a nitrogen atom to which they are attached may form an aliphatic nitrogenated heterocyclic group; X represents a methine group or a nitrogen atom; Y represents -CH2-O-, -CH=CH- or the like; Z1 represents a single bond, a C1-4 alkylene group or the like; Z2 represents a single bond or a C1-4 alkylene group; L represents a methylene group, a C3-8 cycloalkylene group or the like; and Ar represents an aromatic carbocyclic group or the like. The compound is useful as a pharmaceutical for a central nerves system disease, a cardiovascular disease or a metabolic disease.
