Discovery of 3-aminopiperidines as potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitors

Jason M. Cox,Bart Harper,Anthony Mastracchio,Barbara Leiting,Ranabir Sinha Roy,Reshma A. Patel,Joseph K. Wu,Kathryn A. Lyons,Huaibing He,Shiyao Xu,Bing Zhu,Nancy A. Thornberry,Ann E. Weber,Scott D. Edmondson

Bioorganic & Medicinal Chemistry Letters（2007）

引用 31|浏览23

暂无评分

摘要

Substituted 3-aminopiperidines 3 were evaluated as DPP-4 inhibitors. The inhibitors showed good DPP-4 potency with superb selectivity over other peptidases (QPP, DPP8, and DPP9). Selected DPP-4 inhibitors were further evaluated for their hERG potassium channel, L-type calcium channel, Cyp2D6, and pharmacokinetic profiles.

查看译文

关键词

Dipeptidyl peptidase IV,DPP-4,DPP8,DPP9,QPP,Aminopiperidine

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