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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