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
  • 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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