新型芳基丙烯酸酯的合成及生物活性

Synthesis and Bioactivity of Novel Aryl Acrylates

依据活性亚结构的拼接原理,以Baylis-Hillman加成物为原料,设计并合成了5种新的芳基丙烯酸酯类化合物,经IR、1HNMR和元素分析测试技术确证;温室条件下测试了目标化合物的生物活性。结果发现,这些化合物在600ga.i./hm2的剂量下对供试靶标无杀虫活性;在400ga.i./hm2的剂量下对供试靶标无杀菌活性;在2000ga.i./hm2的剂量下,对阔叶杂草百日草(YOA)、苘麻(VEL)和禾本科杂草稗草(BYG)、马唐(CRG)均具有一定的除草活性。这些化合物结构全新,分子中具有多个可供修饰的基团,可作为除草活性的新型先导化合物提供进一步的优化。

Five novel aryl acrylates were synthesized from Baylis-Hillman adducts according to the principle of combination of bioactive substructures. Their structures were confirmed by IR, ^1H NMR and elemental analysis. Preliminary bioactivities of these new compounds were evaluated in the green house. The result indicates that the target compounds have no insecticidal activity at 600 g a. i./hm^2 and no fungicidal activity at 400 g a. i./hm^2. The target compounds show certain herbicidal activity against Zinnia elegans Jacq. , Abutilon theophrasti Medic. , Echinochloa crusgalli （L.） Baeuv. and Digitaria sanguinalis （L.） Scop at 2 000 g a. i./hm^2. These compounds are brand new and contain versatile muhifunctional molecules that could easily be modified and used as lead compounds for further study.