| 咪唑啉酮类簇合物的合成及其除草活性 |
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| 引用本文： | 马洪菊,曹坳程,梅向东,宁君,李永红.咪唑啉酮类簇合物的合成及其除草活性[J].农药学学报,2009,11(2):176-180. |
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| 作者姓名： | 马洪菊 曹坳程 梅向东 宁君 李永红 |
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| 作者单位： | 1.农业部农药化学与应用重点开放实验室, 中国农业科学院 植物保护研究所，北京 100193 |
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| 基金项目： | 863 High-tech Key Project of China，The Major State Basic Research Development Program of China，Agricultural Public Sector Reasearch and Special Funds |
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| 摘 要： | 在生物体系中,二效价配体比单效价配体对受体有更强的亲和力。根据乙酰乳酸合成酶与咪唑啉酮类复合物的3D结构信息特点,设计并合成了8个对称的双甲基咪草烟类化合物,其结构经红外、核磁及元素分析等确证。初步生物活性测定结果表明:咪唑啉酮二效价簇合物对乙酰乳酸合成酶的亲和力没有增加,在100 μg/mL浓度下,对油菜Brassica campestris L. 根长抑制率与单效价化合物相当。
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| 关 键 词： | 多位点结合 簇合效应 合成 双甲基咪草烟 |
Synthesis and Bio-activity of Bivalent Imidazolinones |
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| MAHong-ju,CAOAo-cheng,MEIXiang-dong,NINGJun and LIYong-hong.Synthesis and Bio-activity of Bivalent Imidazolinones[J].Chinese Journal of Pesticide Science,2009,11(2):176-180. |
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| Authors: | MAHong-ju CAOAo-cheng MEIXiang-dong NINGJun and LIYong-hong |
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| Institution: | 1.Key Laboratory of Pesticide Chemistry and Application,Ministry of Agriculture,Institute of Plant Protection,Chinese Academy of Agricultural Sciences,Beijing 100193,China2.State Key Laboratory of Elemento Organic Chemistry，National Pesticide Engineering Research Center，Nankai University，Tianjin 300071，China |
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| Abstract: | In biological system, bivalent ligands often possess increased functional affinity for their receptors compared with monovalent ligands. Based on the information of 3D structure of AHAS-imazaquin(IQ) complex,8 symmetrical bivalent molecules of imazapic were designed and synthesized. Their structures were confirmed by IR, 1H NMR and elementary analysis. The preliminary bioassay results showed that the inhibition rate to the acetohydroxyacid synthase from dimeric compounds were less potent than that of imazapic. And the inhibition rate to the growth of rape (Brassica campestris L.) root from bivalent compounds were very close to that of imazapic at concentration of 100 μg/mL. |
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| Keywords: | multivalent interactions cluster effect synthesis bis-imazapic |
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