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姜黄素嘧啶酮衍生物的合成及杀螨活性
引用本文:罗金香,丁伟,张永强,杨振国,李阳.姜黄素嘧啶酮衍生物的合成及杀螨活性[J].农药学学报,2011,13(4):415-418.
作者姓名:罗金香  丁伟  张永强  杨振国  李阳
作者单位:1.西南大学 植物保护学院,重庆 400715
基金项目: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48 h后,活性最好的4,6-二 -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200.3 mg/L,其毒力约为姜黄素的4倍;而处理72 h后,化合物 3a 对朱砂叶螨的LC50值为40.7 mg/L,其毒力约为姜黄素的14倍。

关 键 词:姜黄素    嘧啶酮衍生物    合成    杀螨活性
收稿时间:2010/2/16 0:00:00
修稿时间:2011/2/16 0:00:00

Synthesis and acaricidal activity of curcumin pyrimidinone derivatives
LUO Jin-xiang,DING Wei,ZHANG Yong-qiang,YANG Zhen-guo and LI Yang.Synthesis and acaricidal activity of curcumin pyrimidinone derivatives[J].Chinese Journal of Pesticide Science,2011,13(4):415-418.
Authors:LUO Jin-xiang  DING Wei  ZHANG Yong-qiang  YANG Zhen-guo and LI Yang
Institution:1.College of Plant Protection, Southwest University, Chongqing 400715, China
Abstract: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 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.
Keywords:curcumin  pyrimidinone derivatives  synthesis  acaricidal activity
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