Sar Of Heterocyclic Core Analogs Of A Direct Thrombin Inhibitor
Bioorganic & Medicinal Chemistry Letters(2012)
摘要
Thrombin is a serine protease that plays a key role in blood clotting. Pyrrolidine 1 is a potent thrombin inhibitor discovered at Merck several years ago. Seven analogs (2–8) of 1 in which the pyrrolidine core was replaced with various heterocycles were prepared and evaluated for activity against thrombin, clotting factors VIIa, IXa, Xa, and XIIa, and trypsin. The thiomorpholine analog 6 was the most active, essentially matching the thrombin inhibitory activity of 1 with slightly improved selectivity over trypsin.
更多查看译文
关键词
Thrombin inhibitor,DTI,Thrombosis,Anti-thrombotic
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