Potent, selective, and orally efficacious antagonists of melanin-concentrating hormone receptor 1

FX Tavares, KA Al-Barazanji, EC Bigham…

文献索引：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.; Handlon, Anthony L.; Hertzog, Donald L.; Ignar, Diane M.; Lang, Daniel G.; Ott, Ronda J.; Peat, Andrew J.; Zhou, Hui-Qiang Journal of Medicinal Chemistry, 2006 , vol. 49, # 24 p. 7095 - 7107

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被引用次数: 39

摘要

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 molecule 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 ...