Novel potent and selective thrombin inhibitors based on a central 1,4-benzoxazin-3(4H)-one scaffold

被引：30
|
作者：
Ilas, Janez [1 ]
Tomasic, Tihomir [1 ]
Kikelj, Danijel [1 ]
机构：
[1] Univ Ljubljana, Fac Pharm, Ljubljana 1000, Slovenia
来源：
JOURNAL OF MEDICINAL CHEMISTRY | 2008年 / 51卷 / 09期
关键词：
D O I：
10.1021/jm701622y
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Novel thrombin inhibitors with the central 1,4-benzoxazine-3(4H)-one scaffold, benzamidine P-1 arginine side chain mimetic and various P-3 moieties are described. 3-(Benzyl(2-(4-carbamimidoylbenzyl)-4-methyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-7-yl)amino)-3-oxopropanoic acid (7b), the most potent compound in the series, exhibited a K-i of 2.6 nM in vitro for thrombin and high selectivity against trypsin and factor Xa.
引用
收藏
页码：2863 / 2867
页数：5
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