Eric Bigham - Potent, Selective, and Orally Efficacious Antagonists of Melanin-Concentrating Hormone Receptor 1

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      Publication Details (including relevant citation   information):

      By Tavares, Francis X.; Al-Barazanji, Kamal A.; Bigham, Eric C.;   Bishop, Michael J.; Britt, Christy S.; Carlton, David L.;   Feldman, Paul L.; Goetz, Aaron S.; Grizzle, Mary K.; Guo, Yu   C.;  et al

      From Journal of Medicinal Chemistry (2006), 49(24), 7095-7107.  


      The high expression of MCH in the hypothalamus with the lean   hypophagic phenotype coupled with increased resting metabolic   rate and resistance to high fat diet-induced obesity of MCH KO   mice has spurred considerable efforts to develop small mol. MCHR1   antagonists. Starting from a lead thienopyrimidinone series,   structure-activity studies at the 3- and 6-positions of the   thienopyrimidinone core afforded potent and selective MCHR1   antagonists with representative examples having suitable   pharmacokinetic properties. Based on structure-activity   relationships, a structural model for MCHR1 was constructed.

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