From selective substrate analogue factor Xa inhibitors to dual inhibitors of thrombin and factor Xa.: Part 3
From selective substrate analogue factor Xa inhibitors to dual inhibitors of thrombin and factor Xa.: Part 3
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DOI：
10.1016/j.bmcl.2007.03.105
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发表时间：
2007-06-15
影响因子：
2.7
通讯作者：
Steinmetzer, Torsten
中科院分区：
文献类型：
--
作者：
Doennecke, Daniel;Schweinitz, Andrea;Steinmetzer, Torsten
高效和选择性的底物类似物因子Xa抑制剂通过掺入从凝血酶抑制剂的开发中已知的非碱性或适度碱性PI残基而获得。P2和P3氨基酸的修饰强烈影响选择性，并提供有效的双重因子Xa和凝血酶抑制剂，而不影响纤溶酶。几种抑制剂在人血浆中的标准凝血试验中表现出优异的抗凝效力。(c)2007爱思唯尔有限公司保留所有权利。
Highly potent and selective substrate analogue factor Xa inhibitors were obtained by incorporation of non-basic or modestly basic PI residues known from the development of thrombin inhibitors. The modification of the P2 and P3 amino acids strongly influenced the selectivity and provided potent dual factor Xa and thrombin inhibitors without affecting the fibrinolytic enzymes. Several inhibitors demonstrated excellent anticoagulant efficacy in standard clotting assays in human plasma. (c) 2007 Elsevier Ltd. All rights reserved.