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The discovery and optimization of pyrimidinone-containing MCH R1 antagonists |
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| Authors: | Hertzog Donald L Al-Barazanji Kamal A Bigham Eric C Bishop Michael J Britt Christy S Carlton David L Cooper Joel P Daniels Alex J Garrido Dulce M Goetz Aaron S Grizzle Mary K Guo Yu C Handlon Anthony L Ignar Diane M Morgan Ronda O Peat Andrew J Tavares Francis X Zhou Huiqiang |
| Institution: | 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 |
| 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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