7 羟基 4 甲基香豆素衍生物杀螨活性研究

为提高7 羟基 4 甲基香豆素（羟甲香豆素）的杀螨活性,以羟甲香豆素为原料,设计合成8种羟甲香豆素衍生物,通过H NMR和¹³C NMR数据分析进行结构表征,并进行体外杀螨活性检测。结果表明,质量浓度为0.5 g/L的3,6,8 三溴 7 羟基 4 甲基香豆素、8 乙酰基 7 羟基 4 甲基香豆素、7 （4 氯苄氧基） 4 甲基香豆素和7 乙酰氧基 4 甲基香豆素在24 h的致螨死亡率分别为100%、73.0%、68.3%和66.2%,与羟甲香豆素比较,差异极显著（P<0.01）;质量浓度为0.5 g/L的7 苯乙氧基 4 甲基香豆素和7 苄氧基 4 甲基香豆素在24 h的致螨死亡率分别为35.5%和34.7%,与羟甲香豆素比较,差异显著（P<0.05）。说明结构修饰是研发高活性羟甲香豆素类杀螨药物的可行途径,这对杀螨新药剂的进一步研究及应用具有重要指导意义。

Synthesis and Acaricidal Activity of 7 Hyderoxy 4 methycomarin Derivatives

In order to improve the acaricidal activity of 7 hydroxy 4 methylcoumarin (hymecromon), eight hymecromone derivatives were synthesized using hymecromon as starting material. and were structurally confirmed by H NMR and ¹³C NMR, and the acaricidal activity of derivatives in vitro was also determined. The results showed that the mortality rates of Psoroptes cuniculi caused by 3,6,8 tribromo 7 hydroxy 4 methylcoumarin, 8 acetyl 7 hydroxy 4 methylcoumarin, 7 (4 chloroben zyloxy) 4 methylcoumarin and 7 exthoxy 4 methylcoumarin groups with mass concentration of 0.5 g/L were 100%, 73.0%, 68.3% and 66.2% respectively within 24 hours, and the difference was extremely significant (P<0.01) compared with hymecromone. The mortality rates caused by 7 phenylethoxy 4 methylcoumarin and 7 benzoxy 4 methylcoumarin groups with mass concentration of 0.5 g/L were 35.5% and 34.7%, respectively, and the difference was significant compared with hymecromon (P<0.05). The results indicated that the structural modification could be a feasible way for developing highly acaricidal activity of hymecromone, and the present results also had profound guiding significance for further research and development of new animal acaricide.