阿魏酸酰腙类化合物的合成及生物活性

将酰腙结构引入到阿魏酸衍生物中,合成了6个阿魏酸酰腙类化合物,其结构经过了IR、~1H NMR、~(13)C NMR和ESI-HRMS表征。抗病毒活性测试结果表明,在质量浓度为500mg/L时,化合物3、5和6对烟草花叶病毒(TMV)在保护、治疗和钝化活性方面的抑制率均优于对照药剂病毒唑。进一步的EC_(50)测试结果表明,化合物3、5和6钝化活性的EC_(50)值分别为91.25、54.86、58.22mg/L,明显低于病毒唑的EC_(50)值(126.05mg/L)。该研究结果表明,阿魏酸酰腙类化合物对TMV具有较好的抗病毒活性,对其进行适当的结构改进和优化,有望得到具有更高抗病毒活性的化合物。

Syntheses and Biological activities of Ferulic Acid Acylhydrazone Compounds

Six compounds were synthesized by introducing acylhydrazone unit into ferulic acid derivatives, and their structures were characterized by IR,1H NMR, 13C NMR and ESI-HRMS. Antiviral activity test results showed that compounds 3, 5, and 6 presented good protective, curative and inactivating activity against TMV, which were superior to the control drug ribavirin at 500 mg/L. The EC50 values of the inactivation activity of compounds 3, 5 and 6 on TMV were 91.25, 54.86, and 58.22 mg/L, which were significantly lower than the EC50 value (126.05 mg/L) of ribavirin. The results indicated that ferulic acid derivatives containing acylhydrazone moiety had potent antiviral activity against TMV. It is expected that compounds with higher antiviral activity can be obtained after proper structural improvement and optimization.