阿魏酸酰腙类化合物的合成及抗病毒活性  

Synthesis and antiviral activity of trans-ferulic acid derivatives containing acylhydrazone moiety

作　　者：王珍珍 王晓斌 金林红 WANG Zhen-zhen;WANG Xiao-bin;JIN Lin-hong(Rice Institute of Guizhou Province,Guiyang 550006,China;Jiangsu Key Laboratory of Pesticide Science,Nanjing Agricultural University,Nanjing 210095,China;State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering,Key Laboratory of Green Pesticide and Agricultural Bioengineering,Ministry of Education,Center for Research and Development of Fine Chemicals, Guizhou University,Guiyang 550025,China)

机构地区：[1]贵州省水稻研究所,贵州贵阳550006 [2]江苏省农药学重点实验室,南京农业大学,江苏南京210095 [3]绿色农药与农业生物工程国家重点实验室培育基地,教育部绿色农药与生物工程重点实验室,贵州大学精细化工研究开发中心,贵州贵阳550025

出　　处：《化学研究与应用》2020年第7期1227-1233,共7页Chemical Research and Application

基　　金：国家自然科学基金重点项目(21132003)资助;贵州省优质特色水稻研发与转化及园区技术服务能力建设项目(黔科合平台人才[2017]5719)资助。

摘　　要：以天然产物阿魏酸为先导结构,设计合成了一系列反式阿魏酸酰腙类化合物,以烟草花叶病毒(TMV)为研究对象,对目标化合物进行抗病毒活性测试。该系列目标化合物结构经IR,1H NMR,13C NMR和HRMS确证,生物活性测试结果表明:在药剂质量浓度为500 mg·L-1时,绝大部分化合物对烟草花叶病毒具有较好的抑制活性。反式阿魏酸酰腙类化合物对烟草花叶病毒具有较好的抑制作用,在其结构基础上进行一定的结构修饰,有望得到具有较高抗病毒活性的化合物。Using the structure of trans-ferulic acid as molecular template,a series of ferulic acid derivatives containing acylhydrazone moiety were designed,synthesized,and systematically evaluated for their antiviral activity in vivoagainst tobacco mosaic virus(TMV).The structures of target compounds were characterized by IR,1H NMR,13C NMR and HRMS.Meanwhile,the bioassay tests demonstrated that most of the title compounds exhibited desirable antiviral activity against TMV at 500 mg·L-1.Trans-ferulic acid derivatives containing acylhydrazone fragment showed potent antiviral activity against TMV and were expected to be further modified for obtaining compounds with higher antiviral activity.

关 键 词：阿魏酸 酰腙 烟草花叶病毒 抗病毒活性 

分 类 号：O626.2[理学—有机化学]