丙烯酸酯衍生物的设计、合成及生物活性

Design, synthesis and bioactivity activity of acrylate derivatives

[目的]寻找较高杀菌活性的丙烯酸酯类化合物。[方法]利用Baylis-Hillman加成物及其衍生物与活性杂环化合物进行拼接,设计合成一系列新型丙烯酸酯衍生物。[结果]合成了4类27个丙烯酸酯衍生物,所合成的化合物经^(1)H NMR和元素分析确证,并初步测定了其杀菌活性。[结论]杀菌活性测试结果表明:部分目标化合物对黄瓜霜霉病具有一定的活性,并且目标化合物分子中具有多个可供修饰的基团,可以作为生物活性的片段或新型先导化合物供进一步优化研究。

[Aims] This study aims to search for novel acrylates with higher fungicidal activity. [Methods] A series of new acrylate derivatives were designed and synthesized using Baylis-Hillman adducts and their derivatives spliced with active heterocyclic compounds. [Results] 27 Acrylate derivatives of 4 classes were synthesized. The target compounds were confirmed by^(1)H NMR and elemental analysis, and their fungicidal activities were initially screened.[Conclusions] The results of the fungicidal activity tests showed that some of the target compounds have certain activity against cucumber downy mildew(CDM), the target compound molecules have multiple groups available for modification, and can be used as biologically active fragments or novel lead compounds for further optimization studies.