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新型3-(α-羟基吲哚亚甲基)吡咯烷-2,4-二酮衍生物的合成与除草活性研究
Synthesis and Bioactivities of Novel 3-α-Hydroxy(indol-3-yl)-methylene-pyrrolidine-2,4-dione Derivatives
【摘要】 为了进一步研究3-羟亚甲基吡咯烷-2,4-二酮类化合物构效关系,以期发现高活性化合物,利用生物等排原理引入具有芳香性的吲哚环,合成了22个未见文献报道的新型3-羟亚甲基吡咯烷-2,4-二酮衍生物,其结构均经过1HNMR和元素分析确证.初步生物活性测试结果表明,这些化合物均具有一定的除草活性.初步的构效关系研究表明,该类吡咯烷-2,4-二酮类化合物的除草活性与平面A和B的相对构型有关.
【Abstract】 In order to further study the structure-activity relationships of the title compounds and find new kinds of herbicides,the aromatic indole ring was introduced and 22 new compounds were prepared by reaction of ketoacid esters with amio-acid esters.All of them have been confirmed by 1H NMR spectra and elemental analysis.The preliminary bioassay results indicated that all of them possessed some extent herbicidal activities.Preliminary quantitative structure-activity relationship (QSAR) analysis indicated that the herbicidal activity for pyrrolidine-2,4-dione derivatives was strongly related with the configuration for planes A and B.
【Key words】 indole； pyrrolidine-2,4-dione； synthesis； herbicidal activity； quantitative structure-activity relationship；
- 【文献出处】 有机化学 ,Chinese Journal of Organic Chemistry , 编辑部邮箱 ,2010年08期
- 【分类号】O626
- 【被引频次】12
- 【下载频次】323