2. Academic Validation
  3. The discovery and optimization of pyrimidinone-containing MCH R1 antagonists

The discovery and optimization of pyrimidinone-containing MCH R1 antagonists

  • Bioorg Med Chem Lett. 2006 Sep 15;16(18):4723-7. doi: 10.1016/j.bmcl.2006.07.008.
Donald L Hertzog 1,  Kamal A Al-Barazanji,  Eric C Bigham,  Michael J Bishop,  Christy S Britt,  David L Carlton,  Joel P Cooper,  Alex J Daniels,  Dulce M Garrido,  Aaron S Goetz,  Mary K Grizzle,  Yu C Guo,  Anthony L Handlon,  Diane M Ignar,  Ronda O Morgan,  Andrew J Peat,  Francis X Tavares,  Huiqiang Zhou
Affiliations

Affiliation

  • 1 Metabolic and Viral Diseases Centre of Excellence for Drug Discovery, GlaxoSmithKline, Five Moore Drive, Research Triangle Park, NC 27707, USA. Donald.L.Hertzog@gsk.com
PMID: 16870432 DOI: 10.1016/j.bmcl.2006.07.008
Abstract

Optimization of a series of constrained melanin-concentrating hormone receptor 1 (MCH R1) antagonists has provided compounds with potent and selective MCH R1 activity. Details of the optimization process are provided and the use of one of the compounds in an animal model of diet-induced obesity is presented.

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