中文摘要：

本研究以灯盏乙素苷元,N-取代氨甲基苯甲酸以及6-取代烟酸为原料,在偶联剂DCC/DMAP的作用下经4步反应制备了灯盏乙素苷元4＇-N-取代氨甲基苯甲酸酯-7-取代烟酸酯衍生物1a~1f,并经1H NMR,ESI-MS以及HRMS确证结构。对化合物1a~1f进行了神经细胞氧化损伤保护活性与理化性质研究,结果显示,烟酸酯结构的引入能够提高化合物抗氧化活性以及水溶性,其中化合物1d具有较高的水溶性、体外稳定性及抗氧化活性,值得进一步研究。

英文摘要：

4＇-N-substituted aminomethylbenzoate-7-substituted nicotinic acid ester derivatives of scutellarein （1a - 1f） were prepared in four steps from scutellarein, N-substituted aminomethylbenzoic acid and 6-substituted nicotinic acid in the presence of N,N＇-dicyclohexylcarbodiimide （DCC）/4-dimethylaminopyridine （DMAP）. The structures of compounds 1a - 1f were confirmed by IH NMR, ESI-MS and HRMS. Physicochemical properties and in vitro antioxidant activities were evaluated. The results showed that incorporation of nicotinic ester group at 7-position of 4＇-N-substituted aminomethylbenzoate derivatives of scutellarein could enhance in vitro antioxidant activities and aqueous solubility. Compound ld had higher solubility, stability and antioxidant activity deserved further research.