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

页码：2863 / 2867

页数：5

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