有机化学 ›› 2003, Vol. 23 ›› Issue (6): 550-554. 上一篇    下一篇

研究论文

1-芳基-1,4二氢-3芳酰肼基甲酰基-6甲基-4-哒嗪酮的合成及对黄瓜子叶生根作用的构效关系研究

邹霞娟;来鲁华;金桂玉;黄桂琴   

  1. 北京大学化学与分子工程学院物理化学研究所;南开大学化学学院元素有机研 究所
  • 发布日期:2003-06-25

Synthesis, Plant Growth Regulating Effect and QSAR of a Series of 1- Aryl-1,4-dihydro-3-acylhydrazinocarbonyl-6-methyl-4-pyridazinones

Zou Xiajuan;Lai Luhua;Jin Guiyu;Huang Guiqin   

  1. Satte key Laboratory for Structural Chemistry Studies of Stable and Unstable Species,Isntitute of Physical Chemistry,College of Chemistry and Molecular Engineering,peking University;National Key laboratory of Elemento-Organic Chemistry,Institute of elemento-Organic Chemistry, Nankai University
  • Published:2003-06-25

合成了一系列的1-芳基-1,4-二氢-3-芳酰肼基甲酰基-各甲基斗哒嗪酮类化合 物,并用离体黄瓜子叶生根法测试其生物活性,生测结果表明,所有的化合物均显 示出一定的生物活性,并且芳环上的取代基对活性有重要影响.采用化合物的物理 化学参数及化合物促进黄瓜子叶生根的活性,进行了结构与活性定量关系研究,建 立了较好的结构与活性的相关式,化合物的亲脂性和取代基的电性对化合物的生物 活性具有重要的影响.研究结果对3-芳酰肼基甲酰基斗哒嗪酮类化合物的改性或新 类似物的合成具有指导意义.

关键词: 酰肼 P, 哒嗪酮 P, 植物生长条件剂, 构效关系, 生物活性

A series of 1-atyl-l, 4-dihydro-3-acylhydrazinocarbonyl-6-methyl-4- pyridazinones, related to the plant growth regulating effect (GRE), were synthesized and tested in excised Cucumber cotyledon root- formation. The bioassay shows that the tide compounds possess promoting Cucumber cotyledon root-formation activity. And the activity was influenced by the nature of the substituents. The quantitative relationship between the structure of the compounds and their GRE activity was analyzed, using the physicochemical parameters of the substituents and regression analyzed. The result shows that both hydrophobic parameter and electronic parameter of the substituents are the major one in affecting the activity. This offers important structural insights into designing highly active compounds prior to their synthesis.

Key words: HYDRAZIDE P;PYRIDAZINONE P;PLANT GROWTH REGULATORS, STRUCTURE ACTIVITY RELATIONSHIP;BIOLOGICAL ACTIVITY

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