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Novel benzimidazole-based MCH R1 antagonists |
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| Authors: | Carpenter Andrew J Al-Barazanji Kamal A Barvian Kevin K Bishop Michael J Britt Christy S Cooper Joel P Goetz Aaron S Grizzle Mary K Hertzog Donald L Ignar Diane M Morgan Ronda O Peckham Gregory E Speake Jason D Swain Will R |
| Affiliation: | Metabolic and Viral Diseases Centre of Excellence for Drug Discovery, GlaxoSmithKline, Five Moore Drive, Research Triangle Park, NC 27709, USA. andrew.j.carpenter@gsk.com |
| Abstract: | The identification of an MCH R1 antagonist screening hit led to the optimization of a class of benzimidazole-based MCH R1 antagonists. Structure-activity relationships and efforts to optimize pharmacokinetic properties are detailed along with the demonstration of the effectiveness of an MCH R1 antagonist in an animal model of obesity. |
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