2. Academic Validation
  3. Discovery of novel phenethylpyridone derivatives as potent melanin-concentrating hormone 1 receptor antagonists

Discovery of novel phenethylpyridone derivatives as potent melanin-concentrating hormone 1 receptor antagonists

  • Bioorg Med Chem Lett. 2009 Sep 1;19(17):5186-90. doi: 10.1016/j.bmcl.2009.07.023.
Makoto Ando 1,  Etsuko Sekino,  Yuji Haga,  Minoru Moriya,  Masahiko Ito,  Junko Ito,  Hisashi Iwaasa,  Akane Ishihara,  Akio Kanatani,  Norikazu Ohtake
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, Tsukuba Research Institute, Merck Research Laboratories, Banyu Pharmaceutical Co. Ltd, Okubo-3, Tsukuba, Ibaraki, Japan. andoumkt@gmail.com
PMID: 19632840 DOI: 10.1016/j.bmcl.2009.07.023
Abstract

Novel phenethylpyridone derivatives were identified as potent human melanin-concentrating hormone 1 receptor (MCH-1R) antagonists. A search for surrogates for the 4-(2-aminoethoxy)phenyl moiety of 1 resulted in discovery of 2-[4-(aminomethyl)phenyl]ethyl substructure as in 6a. Successive optimization of the right-hand moiety led to the identification of a number of potent derivatives.

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