新型二硫杂环戊烯硫酮化合物的合成及其对谷氨酸诱导损伤HT22细胞的保护作用

在保留ADT-OH的3H-1,2-二硫杂环戊烯-3-硫酮结构的基础上，用芳乙烯基替换4-羟基苯环，设计并合成了6个二硫杂环戊烯硫酮化合物（L₁~L₆,其中L₂, L₃, L₅和L₆为新化合物），其结构经¹H NMR, ¹³C NMR和HR-MS(ESI)表征。采用MTT法研究了L₁~L₆对谷氨酸诱导损伤的海马神经元HT22细胞的影响。药理初筛结果表明:给药浓度为10~100 μmol·L^-1时，L₁, L₂, L₄和L₆均能提高受损HT22细胞的存活率(P<0.01)；给药浓度为1 μmol·L^-1时，L₃和L₅均可提高损伤HT22细胞的存活率(P<0.01)。

Synthesis of Novel 3H-1,2-dithiole-3-thione Compounds and Their Protective Effects on Glutamic Acid-induced Damage of HT22 Cells

The structure of ADT-OH was modified by replacing 4-OH phenyl with aryl vinyl, based on retaining its 3H-1,2-dithiocyclopentene-3-thione.Six 3H-1,2-dithiole-3-thione compounds(L1~L6) were designed and synthesized.Among them, L2, L3, L5 and L6 were novel compounds.The structures were characterized by 1H NMR, 13C NMR and HR-MS(ESI).Effects of L1~L6 on glutamic acid-induced damage of HT22 cells were investigated by MTT method.The primary pharmacological results displayed that L1, L2, L4 and L6 significantly improved the survival rates of damaged HT22 cells at the concentration of 10~100 μmol·L-1(P<0.01), L3 and L5 increased the survival rates of damaged HT22 cells at the concentration of 1 μmol·L-1(P<0.01).