Synthesis of heparin-like antithrombotics having perphosphorylated thrombin binding domains

被引：14

作者：

Buijsman, RC

Basten, JEM

Dreef-Tromp, CM

van der Marel, GA

van Boeckel, CAA

van Boom, JH

机构：

[1] Leiden Inst Chem, Gorlaeus Labs, NL-2300 RA Leiden, Netherlands

[2] NV Organon, Lead Discovery Unit, NL-5340 BH Oss, Netherlands

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 1999年 / 7卷 / 09期

关键词：

antithrombotics; enzyme inhibitor; heparin; oligosaccharides; thrombin;

D O I：

10.1016/S0968-0896(99)00139-X

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The synthesis of three heparin analogues (i.e. compounds VI-VIII) having perphosphorylated thrombin binding domains (TBDs) is reported. These compounds were tested in vitro for their antithrombin III (ATIII)-mediated anti-Xa and antithrombin activities. Conjugates VI and VIII show a remarkable increase in antithrombin activity compared to the structurally related conjugates with persulfated TBDs (i.e. compounds IV and V), whereas compound VII displays a diminished activity. (C) 1999 Elsevier Science Ltd. All rights reserved.

引用

收藏

页码：1881 / 1890

页数：10

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