Tricyclic dihydroquinazolinones as novel 5-HT 2C selective and orally efficacious anti-obesity agents

…, C Hung, S Malmstrom, G Zhang, E O'Tanyi…

文献索引：Ahmad, Saleem; Ngu, Khehyong; Miller, Keith J.; Wu, Ginger; Hung, Chen-pin; Malmstrom, Sarah; Zhang, Ge; O'Tanyi, Eva; Keim, William J.; Cullen, Mary Jane; Rohrbach, Kenneth W.; Thomas, Michael; Ung, Thao; Qu, Qinling; Gan, Jinping; Narayanan, Rangaraj; Pelleymounter, Mary Ann; Robl, Jeffrey A. Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 3 p. 1128 - 1133

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被引用次数: 10

摘要

Agonists of the 5-HT2C receptor have been shown to suppress appetite and reduce body weight in animal models as well as in humans. However, agonism of the related 5-HT2B receptor has been associated with valvular heart disease. Synthesis and biological evaluation of a series of novel and highly selective dihydroquinazolinone-derived 5-HT2C agonists with no detectable agonism of the 5-HT2B receptor is described. Among these, ...