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

Kevin K-C Liu,Bruce A Lefker,Mark A Dombroski,Phoebe Chiang,Peter Cornelius,Terrell A Patterson,Yuan Zeng,Stephanie Santucci,Elizabeth Tomlinson,Colleen P Gibbons,Ravi Marala,Janice A Brown,Jimmy X Kong,Eunsun Lee,Wendy Werner,Zane Wenzel,Craig Giragossian,Hou Chen,Steven B Coffey

Bioorganic & Medicinal Chemistry Letters（2010）

引用 10|浏览48

暂无评分

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.

查看译文

关键词

5HT2c agonist,Obesity,Binding selectivity

AI 理解论文

溯源树

样例

生成溯源树，研究论文发展脉络

Chat Paper

正在生成论文摘要