7-羟基-4-甲基香豆素衍生物杀螨活性研究  

Synthesis and Acaricidal Activity of 7-Hyderoxy-4-methycomarin Derivatives

作　　者：周泐[1] 尚丛珊[1] 宋晓平[1] 

机构地区：[1]西北农林科技大学动物医学院,中兽医药研究所,陕西杨凌712100

出　　处：《西北农业学报》2013年第10期39-43,共5页Acta Agriculturae Boreali-occidentalis Sinica

基　　金："十一五"国家科技支撑计划项目(2008BADB4B05)

摘　　要：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1 H-NMR和13 C-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0.5g/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24h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0.5g/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24h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。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 1H 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-zy- loxy）- 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 ex tremely significant （P〈0.01） compared with hymecromone. The mortality rates caused by 7-phenyle- thoxy-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 develo- ping highly acaricidal activity of hymecromone, and the present results also had profound guiding sig- nificance for further research and development of new animal acaricide.

关 键 词：羟甲香豆素衍生物 兔痒螨 杀螨活性 

分 类 号：TQ24[化学工程—有机化工]