Synthesis and structure-activity relationships of retro bis-aminopyrrolidine urea (rAPU) derived small-molecule antagonists of the melanin-concentrating hormone receptor-1 (MCH-R1). Part 2.

Sarah Hudson,Mehrak Kiankarimi,Martin W Rowbottom,Troy D Vickers,Dongpei Wu,Joseph Pontillo,Brett Ching,Wesley Dwight,Val S Goodfellow,David Schwarz,Christopher E Heise,Ajay Madan,Jenny Wen,William Ban,Hua Wang,Warren S Wade

Bioorganic & Medicinal Chemistry Letters（2006）

引用 19|浏览22

暂无评分

摘要

The design, synthesis, and SAR of a series of retro bis-aminopyrrolidine ureas are described. Compounds from this series exhibited considerable binding affinity (Ki=1nM) and functional activity at MCH-R1, acceptable CYP2D6 inhibition, and good rat brain exposure.

查看译文

关键词

Retro bis-aminopyrrolidine urea,Melanin-concentrating hormone receptor-1,Antagonists,CYP2D6

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