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[低分子量肝素模拟物的合成]

[Synthesis of low molecular weight mimetics of heparin].

作者信息

Krylov V B, Ustiuzhanina N E, Nifant'ev N E

出版信息

Bioorg Khim. 2011 Nov-Dec;37(6):745-79. doi: 10.1134/s1068162011060100.

Abstract

Natural hexosaminoglycan heparin remains the most commonly prescribed anticoagulant in hospitalized patients. However its administration could induce side clinical events, including thrombocytopenia and bleeding. This explaines the need of development of alternative anticoagulant drugs based on modified heparin and polyanionic oligo- and polysaccharide derivatives, such as sulfated glucans, phosphomannans and fucoidans. Here we review the works on the synthesis of oligosaccharides related to low molecular weight hepain fragments and their derivatives, as well as oligosaccharides, which imitate parts of heparin chain responsible for biological activity. These works were aimed to develop the pharmaceutical preparations lacking ofheparin disadvantages.

摘要

天然己糖胺聚糖肝素仍是住院患者最常用的抗凝剂。然而,其给药可能会引发包括血小板减少和出血在内的不良临床事件。这就解释了为何需要开发基于修饰肝素和聚阴离子寡糖及多糖衍生物(如硫酸化葡聚糖、磷酸甘露聚糖和岩藻依聚糖)的替代抗凝药物。在此,我们综述了与低分子量肝素片段及其衍生物相关的寡糖以及模拟肝素链中具有生物活性部分的寡糖的合成研究。这些研究旨在开发没有肝素缺点的药物制剂。

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