新型芳基丙烯酸酯的合成及生物活性

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。

Synthesis and Bioactivity of Novel Aryl Acrylates

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./hm2 and no fungicidal activity at 400 g a.i./hm2. 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./hm2. These compounds are brand new and contain versatile multifunctional molecules that could easily be modified and used as lead compounds for further study.