Orally active and brain permeable proline amides as highly selective 5HT2c agonists for the treatment of obesity

…, P Chiang, P Cornelius, TA Patterson, Y Zeng…

文献索引：Liu, Kevin K.-C.; Lefker, Bruce A.; Dombroski, Mark A.; Chiang, Phoebe; Cornelius, Peter; Patterson, Terrell A.; Zeng, Yuan; Santucci, Stephanie; Tomlinson, Elizabeth; Gibbons, Colleen P.; Marala, Ravi; Brown, Janice A.; Kong, Jimmy X.; Lee, Eunsun; Werner, Wendy; Wenzel, Zane; Giragossian, Craig; Chen, Hou; Coffey, Steven B. Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 7 p. 2365 - 2369

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被引用次数: 7

摘要

Brain-penetrable proline amides were developed as 5HT2c agonists with more than 1000- fold binding selectivity against 5HT2b receptor. After medicinal chemistry optimization and SAR studies, orally active proline amides with robust efficacy in a rodent food intake inhibition model were uncovered.