中文摘要：

目的：研究灯盏乙素苷元4’-N，N-双取代氨甲基苯甲酸醚类衍生物的合成方法及其对PCI2细胞的保护作用。方法：以灯盏乙素苷元为原料，通过缩合反应、酰氯反应等，经乙酰氯／甲醇体系脱去保护基后获得灯盏乙素苷元4’N，N-双取代氨甲基苯甲酸醚类衍生物（8a～8f）；采用MTT及LDH漏出率法研究化合物对PCI2细胞的保护作用。结果：合成的化合物能较强抑制PCI2细胞所受的氧化损伤，其中化合物8e，8f对PCI2细胞的保护作用显著优于阳性对照药维生素E8e，8f分别为（40．87±1．12），（41．734-0．61），VE为（45．61±0．82），P〈0．05，结论：合成方法方便可行，灯盏乙素苷元4’-N，N-双取代氨甲基苯甲酸醚类衍生物有较好的体外活性，具有进一步开发前景。

英文摘要：

Objective： To synthesis 4＇-N, N-Bis-substituted （aminomethyl） benzoate ether derivatives of scutellarein with improved anti-oxidative activity, and investigation of their protection against nerve cells oxidative damage. Method： Scutellarein 2-bromoethyl ether （4） was synthesized in the presence of 1, 8-diazabicyclo 5.4.0 undec-7-ene （DBU） with scutellarein and 2-bromoethanol as starting materials. N-substituted （aminomethyl） benzoic acids （5a-c） were converted to benzoic chloride （6a-c） by using oxalyl chloride, then the latter coupled with 4 in the presence of 4A MS to obtained compounds （7a-f）, then diphenyl ketal protecting group of the above compounds was removed by using acetic acid chloride/methanol system to obtain target compounds （8a-f） , prodrugs were tested for their cytotoxieity and antioxidant activity in PC12 cells by MTT and LDH leakage rate assay. Result ： The structure of synthesized compounds 8a-f was confirmed by the methods of IH_NMR, ESI- MS. The results indicated that compound 8e and 8f have more potent anti-oxidative activity than positive control Vitamin E. Conclusion： The synthetic method we used has preferable practicality and can be used in synthesizing scutellarein 4＇-N, N-bissubstituted （aminomethyl） benzoate ether derivatives, bioactivity evaluation results suggested that the kind of prodrugs are worthy of further investigation to discover new anti-oxidative agents.