Author/Authors :
Koo Lee، نويسنده , , Won-Hyuk Jung، نويسنده , , Cheol Won Park، نويسنده , , Chang Yong Hong، نويسنده , , In Chul Kim، نويسنده , , Sangsoo Kim، نويسنده , , Yeong Soo Oh، نويسنده , , O Hwan Kwon، نويسنده , , Sung-Hack Lee، نويسنده , , Hee Dong Park، نويسنده , , Sang Woong Kim، نويسنده , , Yong Hee Lee، نويسنده , , Yung Joon Yoo، نويسنده ,
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.
