4-羟基-3-甲氧基肉桂酸衍生物的除草活性测定

Herbicidal Activity of 4-Hydroxy-3-methoxycinnamic Acid Derivatives

[目的]天然产物4-羟基-3-甲氧基肉桂酸是新型除草剂创制的先导化合物,为了评价其衍生物的除草活性。[方法]试验采用平皿法测定了以4-羟基-3-甲氧基肉桂酸为母体合成的26种衍生物对拟南芥的抑制作用。[结果]17种衍生物具有不同程度的除草活性,其中2-(4-羟基-3-甲氧基亚苄基)丙二酸二乙酯、N-(4-氟苯基)-3-(4-羟基-3-甲氧基苯基)丙烯酰胺、3-溴-4-羟基-5-甲氧基肉桂酸3种衍生物除草活性较高,对拟南芥的抑制中浓度(IC50)分别为9.90、7.53、6.93 mg/L。[结论]4-羟基-3-甲氧基肉桂酸衍生物是开发新型除草剂的重要来源,为新型除草剂的创制奠定了一定的理论基础。

[Aims]This study aims to evaluate the herbicidal activity of derivatives of 4-hydroxy-3-methoxycinnamic acid,an important lead compound for the discovery of new herbicides.[Methods]The inhibition activity of 26 derivatives from 4-hydroxy-3-methoxycinnamic acid as the mother skeleton was determined by the plate method.[Results]17 Derivatives had certain herbicidal activity,among which three derivatives had higher herbicidal activity,respectively 2-(4-hydroxy-3-methoxybenzylidene)diethyl malonate,N-(4-fluorophenyl)-3-(4-hydroxy-3-methoxyphenyl)acrylamide and 3-bromo-4-hydroxy-5-methoxycinnamic acid,and the inhibitory concentrations(IC50)for Arabidopsis were 9.90,7.53 and 6.93 mg/L,respectively.[Conclusions]4-Hydroxy-3-methoxycinnamic acid derivatives are an important source for the development of new herbicides,laying a theoretical foundation for the discovery of new herbicides.