Matsuoka Koji, Takita Chiharu, Koyama Tetsuo, Miyamoto Daisei, Yingsakmongkon Sangchai, Hidari Kazuya I P J, Jampangern Wipawee, Suzuki Takashi, Suzuki Yasuo, Hatano Ken, Terunuma Daiyo
Area for Molecular Function, Division of Material Science, Graduate School of Science and Engineering, Saitama University, Sakura, Saitama 338-8570, Japan.
Bioorg Med Chem Lett. 2007 Jul 15;17(14):3826-30. doi: 10.1016/j.bmcl.2007.05.016. Epub 2007 May 13.
A conventional synthesis of alpha-thioglycoside of sialic acid as a glycomonomer was accomplished. Radical copolymerization of the glycomonomer with vinyl acetate proceeded smoothly to afford a new class of glycopolymers having thiosialoside residues, in which all protection was removed by a combination of transesterification and saponification to provide a water-soluble thiosialoside cluster. The results of a preliminary study on biological responses against influenza virus neuraminidases using the thiosialoside polymer as a candidate for a neuraminidase inhibitor showed that the glycopolymer has potent inhibitory activity against the neuraminidases.
完成了作为糖单体的唾液酸α-硫代糖苷的常规合成。该糖单体与醋酸乙烯酯的自由基共聚反应顺利进行，得到了一类具有硫代唾液酸残基的新型糖聚合物，通过酯交换和皂化相结合的方法去除了所有保护基，得到了水溶性硫代唾液酸簇。以硫代唾液酸聚合物作为神经氨酸酶抑制剂候选物对流感病毒神经氨酸酶进行生物反应的初步研究结果表明，该糖聚合物对神经氨酸酶具有强大的抑制活性。
