Benzylamine-based selective and orally bioavailable inhibitors of thrombin.
作者信息
Lee K, Jung W H, Park C W, Hong C Y, Kim I C, Kim S, Oh Y S, Kwon O H, Lee S H, Park H D, Kim S W, Lee Y H, Yoo Y J
机构信息
Biotech Research Institute, LG Chemical Ltd./Research Park, Taejon, Korea.
出版信息
Bioorg Med Chem Lett. 1998 Sep 22;8(18):2563-8. doi: 10.1016/s0960-894x(98)00456-9.
PMID:9873581
Abstract
A series of p-aminomethylphenylalanine derivatives were investigated as novel thrombin inhibitors. This study led to potent inhibitors of thrombin (Ki up to 3.3 nM) that are trypsin-selective, highly orally bioavailable in rats, and highly permeable across Caco-2 cells. The P1 benzylamine binding mode in the thrombin active site was identified by X-ray crystallographic analysis.
摘要
Zotero 插件