Abstract A series of glycosyl-substituted 1,3,4-oxadiazoles were synthesized by cyclization of glycosyl-acylthiosemicarbazides via a base-catalyzed reaction. The starting glycosyl-acylthiosemicarbazide derivatives were obtained by the reaction of glycosyl isothiocyanate with various hydrazides. The acetylcholinesterase (AChE) inhibitory activities of the products were tested by Ellman’s method. The most active compounds were subsequently evaluated for the 50% inhibitory concentration (IC50) values. N-(1,3,4,6-tetra-O-benzyl-2-deoxy-β-D-glucopyranosyl)-5-(4-fluorophenyl)-1,3,4-oxadiazole-2-amine (6i) possesses the best AChE -inhibition activity with an IC50 of 1.61±0.34 μm.

中文翻译：

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作为乙酰胆碱酯酶抑制剂的新型 C2-糖基恶二唑衍生物的合成和生物活性

摘要 通过碱催化反应将糖基-酰基氨基硫脲环化，合成了一系列糖基取代的1,3,4-恶二唑。起始糖基-酰基氨基硫脲衍生物是通过糖基异硫氰酸酯与各种酰肼的反应获得的。产物的乙酰胆碱酯酶(AChE)抑制活性采用Ellman法检测。随后评估了最具活性的化合物的 50% 抑制浓度 (IC50) 值。N-(1,3,4,6-四-O-苄基-2-脱氧-β-D-吡喃葡萄糖基)-5-(4-氟苯基)-1,3,4-恶二唑-2-胺(6i)具有最佳的 AChE 抑制活性，IC50 为 1.61±0.34 μm。