姜黄素嘧啶酮衍生物的合成及杀螨活性  

Synthesis and acaricidal activity of curcumin pyrimidinone derivatives

作　　者：罗金香[1] 丁伟[1] 张永强[1] 杨振国[1] 李阳[1] 

机构地区：[1]西南大学植物保护学院,重庆400715

出　　处：《农药学学报》2011年第4期415-418,共4页Chinese Journal of Pesticide Science

基　　金：重庆市科技攻关项目(CSTC;2008AC1094);西南大学科研基金资助项目(SWU208045);中央高校基本科研业务费专项资金资助(XDJK2010C079);科技部农业科技成果转化基金(2010GB2F100388)

摘　　要：在明确姜黄素具有杀螨活性,且其结构中的双羰基并非是起杀螨作用的关键基团的基础上,设计、合成了4个新颖的姜黄素嘧啶酮衍生物,其结构经红外光谱、核磁共振氢谱和质谱分析确认。生物活性测定结果表明:4个目标化合物均表现出优于母体化合物姜黄素的杀螨活性,处理48h后,活性最好的4,6-二[(E)-4-羟基-3-甲氧基苯丙烯基]-2-嘧啶酮(3a)对朱砂叶螨Tetranychus cinnabarinus和柑橘全爪螨Panoychus cotri的LC50值分别为487.5和200.3mg/L,其毒力约为姜黄素的4倍;而处理72h后,化合物3a对朱砂叶螨的LC50值为40.7mg/L,其毒力约为姜黄素的14倍。Based on the results of previous study,four novel curcumin pyrimidinone derivatives were designed and synthesized.The structures of the new compounds were identified by IR,1H NMR and MS.The acaricidal assay results showed that all four derivatives exhibited higher acaricidal potency than the parent compound.The 48 h LC50 values of 4,6-bis[（E）-4-hydroxy-3-methoxystyryl] pyrimidin-2（1H）-one（3a） with the highest acaricidal potency were 487.5 and 200.3 mg/L to Tetranychus cinnabarinus and Panoychus cotri,respectively.The acaricidal potency of derivatives 3a was about four fold higher than that of curcumin against T.cinnabarinus and P.cotri.Moveover the 72 h LC50 values of 3a was 40.7 mg/L to T.cinnabarinus,which exhibited about fourteen fold higher acaricidal potency than that of curcumin.

关 键 词：姜黄素 嘧啶酮衍生物 合成 杀螨活性 

分 类 号：S482.5[农业科学—农药学]