硫(醇)代α-酮酸酯类化合物的合成及其神经营养活性

Synthesis and Neurotrophic Activities of α-ketothiolester Derivatives

目的 :设计、合成硫 (醇 )代α 酮酸酯类化合物 ,并对其神经营养活性进行初步的评价。方法 :基于先期工作 ,根据功效相关等原理设计、合成硫 (醇 )代α 酮酸酯类化合物 ,并运用体外PC12细胞缺氧存活模型 ,观察了目标化合物的神经营养作用。结果与讨论 :设计、合成硫 (醇 )代α 酮酸酯类化合物 10个 ,其结构经1HNMR、13 CNMR和MS确定。初筛实验结果表明 ,大部分目标化合物对PC12细胞缺氧损伤具有显著的保护作用 ,其具有进一步研究的价值。

AIM: To design and synthesize α-ketothiolester derivatives,and to study their in vitro neurotrophic activities.METHOD:Based on the former work,a series of α-ketothiolester derivatives were designed and synthesized according to the function-activity relationship. To use in vitro successful model for the PC12 cells in anoxic condition,their in vitro neurotrophic activities were observed. RESULT AND CONCLUSION:Ten compounds were designed and synthesized,and their structures were determined by spectral data. The research results showed that most of the compounds have markedly protective effect of anoxic damage of PC12 cells. A further study was worth undertaking.