阿魏酸衍生物的设计、合成及除草活性  

The Design, Synthesis and Herbicidal Activity of Ferulic Acid Derivatives

作　　者：靳丽宇 王明思 田赐 贾然 郝博文 马树杰 董金皋[1] 陈来 张利辉[1] JIN Li-yu;WANG Ming-si;TIAN Ci;JIA Ran;HAO Bo-wen;MA Shu-jie;DONG Jin-gao;CHEN Lai;ZHANG Li-hui(College of Plant Protection,Hebei Agricultural University,Baoding 071000,Hebei,China)

机构地区：[1]河北农业大学植物保护学院,河北保定071000

出　　处：《农药》2021年第3期166-171,共6页Agrochemicals

基　　金：国家重点研发子课题(2017YFD0210304);河北省重点研发项目(19226504D);河北省自然科学基金项目(C2020204036)。

摘　　要：[目的]以天然产物阿魏酸为先导设计合成具有较强除草活性的衍生物。[方法]运用农药分子合理设计原理设计合成阿魏酸酰胺类似物,采用小杯法测定除草活性。[结果]合成了11个新型的阿魏酸衍生物;小杯法测定显示,在400 mg/L质量浓度下,化合物8f和8k的除草活性较好;半抑制浓度测定结果表明:8f对马唐根和茎的IC50值为分别为269.442、344.835 mg/L;8k对反枝苋根和茎的IC50值分别为187.168、224.912 mg/L。[结论]8f和8k具有较强的除草活性,值得进一步研究。[Aims] This study aims to design and synthesize analogs with strong herbicidal activity using, a natural product ferulic acid as the lead compound. [Methods] The method of the rational design principle of pesticide molecules was utilized to design and synthesize ferulic acid amide analogs, and the small cup method was carried out to determine the herbicidal activity. [Results] 11 Derivatives of ferulic acid were synthesized. The results of small cup method showed that at the concentration of 400 mg/L, compound 8f and 8k showed better herbicidal activity. The result showed that IC50 of 8f to the roots and stems of Digitaria sanguinalis were 269.442 and 344.835 mg/L, respectively. The IC50 of 8k to the root and stem of Amaranthus retroflexus were 187.168 and 224.912 mg/L, respectively. [Conclusions] 8F and 8k have strong herbicidal activity, which is worthy of further study.

关 键 词：天然产物 阿魏酸 苯氧乙酸 设计合成 除草剂 

分 类 号：TQ460.3[化学工程—制药化工]