2. Academic Validation
  3. Discovery of novel phenylpyridone derivatives as potent and selective MCH1R antagonists

Discovery of novel phenylpyridone derivatives as potent and selective MCH1R antagonists

  • Bioorg Med Chem. 2011 Jan 15;19(2):883-93. doi: 10.1016/j.bmc.2010.12.002.
Yuji Haga 1,  Sayaka Mizutani,  Akira Naya,  Hiroyuki Kishino,  Hisashi Iwaasa,  Masahiko Ito,  Junko Ito,  Minoru Moriya,  Nagaaki Sato,  Norihiro Takenaga,  Akane Ishihara,  Shigeru Tokita,  Akio Kanatani,  Norikazu Ohtake
Affiliations

Affiliation

  • 1 Tsukuba Research Institute, Banyu Pharmaceutical Co. Ltd, Japan.
PMID: 21190859 DOI: 10.1016/j.bmc.2010.12.002
Abstract

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.

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