Abstract Sulfated polysaccharides and synthetic glycopolymers are promising candidates as antiviral drugs but have failed in clinical trials most likely due to lack of virucidal activity. However, studies have shown that incorporation of lipophilic end groups to oligosaccharide chains is a mean to gain the desired virucidal properties. Here, we describe the introduction of lipophilic end groups to sulfated α- l -fucoside-pendant polymethacrylamides, also known as fucoidan-mimetic glycopolymers, by RAFT polymerization. RAFT agents bearing octadecyl, dioctadecyl and cholesteryl groups were used to synthesize lipoglycopolymers of different chain lengths. Short lipoglycopolymers bearing lipophilic end groups showed an improved ability to block viral entry and infection of cells compared to glycopolymers without lipophilic end groups. Short lipoglycopolymers bearing octadecyl or dioctadecyl end groups, also completely stopped the spreading of the viral infection. However, these lipoglycopolymers did not show actual virucidal properties. Nevertheless, we have described a first step towards obtaining virucidal synthetic glycopolymers for clinical use.

中文翻译：

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通过 RAFT 聚合合成的链端亲脂性岩藻依聚糖模拟糖聚物的抗病毒性能提高

摘要 硫酸化多糖和合成糖聚合物是有前景的抗病毒药物，但在临床试验中很可能由于缺乏杀病毒活性而失败。然而，研究表明，将亲脂性端基并入低聚糖链是获得所需杀病毒特性的一种手段。在这里，我们描述了通过 RAFT 聚合将亲脂性端基引入硫酸化的 α-l-岩藻糖苷侧链聚甲基丙烯酰胺，也称为岩藻依聚糖模拟糖聚合物。带有十八烷基、双十八烷基和胆固醇基团的 RAFT 试剂用于合成不同链长的脂糖聚合物。与没有亲脂性端基的糖聚合物相比，带有亲脂性端基的短脂糖聚合物显示出更好的阻断病毒进入和细胞感染的能力。带有十八烷基或双十八烷基端基的短脂糖聚合物也完全阻止了病毒感染的传播。然而，这些脂糖聚合物并未显示出实际的杀病毒特性。尽管如此，我们已经描述了获得用于临床使用的杀病毒合成糖聚合物的第一步。