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Design and synthesis of a novel synthetic NAPAP-pentasaccharide conjugate displaying a dual antithrombotic action

被引：30
作者：
Buijsman, RC
Basten, JEM
van Dinther, TG
van der Marel, GA
van Boeckel, CAA
van Boom, JH
机构：
[1] NV Organon, Res & Dev Grp, NL-5340 BH Oss, Netherlands
[2] Leiden Univ, Leiden Inst Chem, Gorlaeus Labs, NL-2300 RA Leiden, Netherlands
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 14期
关键词：
D O I：
10.1016/S0960-894X(99)00320-0
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
The synthesis of a novel antithrombotic consisting of a heparin pentasaccharide conjugated to the active site inhibitor N-(2-naphtalenesulfonyl)-glycyl-(D)-4-aminophenyl-alanyl-piperidine(NAPAP) (i.e. compound I) is reported. This conjugate shows a unique pharmacological profile both in vitro and in vivo having direct anti-thrombin and ATIII-mediated anti-Xa activity. Furthermore, conjugate I has a prolonged in vivo half-life compared to NAPAP (1.5 h vs 9 min.), (C) 1999 Elsevier Science Ltd. All rights reserved.
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收藏
页码：2013 / 2018
页数：6
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