Design and synthesis of a novel synthetic NAPAP-penta-saccharide conjugate displaying a dual antithrombotic action.
作者信息
Buijsman R C, Basten J E, van Dinther T G, van der Marel G A, van Boeckel C A, van Boom J H
机构信息
Leiden Institute of Chemistry, Gorlaeus Laboratories, The Netherlands.
出版信息
Bioorg Med Chem Lett. 1999 Jul 19;9(14):2013-8. doi: 10.1016/s0960-894x(99)00320-0.
Abstract
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-piperidin e (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.).
摘要
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