Eleven glycosyl coumarylthiazole derivatives are synthesized by cyclization and condensation of glycosyl thiourea with 3-bromoacetyl coumarins in ethanol. The reaction conditions are optimized and good yields of products (80%–95%) are obtained. The structures of all new products were confirmed by IR, ¹H and ¹³C NMR, and by HRMS (electrospray ionization). The in vitro acetylcholinesterase (AChE) inhibitory activities of these new compounds are tested by Ellman’s method. Among them, N-(2-acetamido-3,4,6-tri-O-acetyl-2-deoxy-β-D-glucopyranosyl)-4-(6-nitrocoumarinyl)-1,3-thiazole-2-amine showed the best activity with an in vitro AChE inhibitory rate of 58% and an IC₅₀ value of 12 ± 0.38 μg/mL.

通过糖基硫脲与3-溴乙酰基香豆素在乙醇中的环化和缩合反应，合成了11种糖基香豆基噻唑衍生物。优化了反应条件，并获得了良好的收率（80％–95％）。所有新产品的结构均通过IR，¹ H和¹³ C NMR以及HRMS（电喷雾电离）确定。在体外乙酰胆碱酯酶抑制这些新化合物的活性由Ellman氏方法进行测试。其中，N-（2-乙酰氨基-3,4,6-三-O-乙酰基-2-脱氧-β - D-吡喃吡喃糖基）-4-（6-硝基香豆基）-1,3-噻唑-2-胺在体外显示出最佳活性AChE抑制率为58％，IC ₅₀值为12±0.38μg/ mL。