摘要/Abstract

设计并合成了一系列1，2，4-三唑-3-硫醚衍生物，目标化合物的化学结构经¹H NMR、¹³C NMR、质谱和元素分析确证；采用单晶X射线衍射法测定了（E）-4-（4-羟基-3-甲氧基苯基亚甲氨基）-5-乙基-4H-1，2，4-三唑-3-丙硫醚（1c）的晶体结构.目标化合物体外神经氨酸酶（Neuraminidase，NA，H1N1）抑制活性测试结果表明，大部分化合物1具有较好的NA抑制活性，其中（E）-4-（4-羟基-3-甲氧基苯基亚甲氨基）-5-乙基-4H-1，2，4-三唑-3-乙硫醚（1b）和1c的NA抑制活性最佳，其IC₅₀值分别为（6.86±2.08）和（9.1±1.56）μg/mL.
关键词: 1,2,4-三唑-3-硫醚衍生物, 合成, 晶体结构, 神经氨酸酶抑制活性
A series of 1,2,4-triazole-3-sulfide derivatives were designed and synthesized. Their chemical structures were confirmed by ¹H NMR, ¹³C NMR, MS and elemental analysis. The crystal structure of (E)-4-(4-hydroxy-3-methoxyphenyl-methyleneamino)-5-ethyl-4H-1,2,4-triazole-3-propylsulfide (1c) was determined by X-ray diffraction analysis. The preliminary assay of neuraminidase (NA, H1N1) inhibitory activity in vitro showed that most of compound 1 has more potent NA inhibitory activity. Among them, compounds (E)-4-(4-hydroxy-3-methoxyphenyl-methyleneamino)-5-ethyl-4H-1,2,4-triazole-3-ethylsulfide (1b) and 1c showed the best inhibitory activity with IC₅₀ values of (6.86±2.08) and (9.1±1.56) μg/mL, respectively.
Key words: 1,2,4-triazole-3-sulfide derivative, synthesis, crystal structure, neuraminidase inhibitory activity


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