INHIBITION OF ACTIVATED PROTEIN-C BY BENZAMIDINE DERIVATIVES

被引：3
|
作者：
STURZEBECHER, J [1 ]
PRASA, D [1 ]
TABY, O [1 ]
机构：
[1] CTR NATL TRANSFUS SANGUINE,F-91943 LES ULIS,FRANCE
来源：
THROMBOSIS RESEARCH | 1993年 / 69卷 / 06期
关键词：
ACTIVATED PROTEIN-C; BENZAMIDINES; INHIBITION; SELECTIVE THROMBIN INHIBITORS;
D O I：
10.1016/0049-3848(93)90057-U
中图分类号：
R5 [内科学];
学科分类号：
1002 ; 100201 ;
摘要：
In studies on the inhibition of activated protein C (APC) by benzamidine derivatives potent inhibitors of APC were found among anilides of 4-amidinophenyl-alpha-aminobutyric acid (K(i) = 0.58 mumol/l). Several bis-benzamidine derivatives containing a cycloalkanone linking bridge inhibit APC with K(i) values near the micromolar range. Potent and selective inhibitors of thrombin derived from 3- and 4-amidinophenylalanine do not inhibit APC. This is of great importance for further development of these inhibitors as potential anticoagulant drugs.
引用
收藏
页码：533 / 539
页数：7
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