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设计合成了一系列文献中未报道的2-取代-6-甲基-4-苯基-3(2H)-哒嗪酮类化合物,其结构经过1H NMR和元素分析确证,化合物4e进行了X射线衍射晶体结构分析.利用油菜平皿法和稗草小杯法对化合物进行了生物活性的测定.初步生物活性测试结果表明,化合物4具有较好的除草活性.定量构效关系表明,化合物4结构中哒嗪环2-位取代基的变化,影响了化合物的抑制活性.当作用对象为油菜时,化合物的活性可能主要与取代基R的立体参数B4和疏水性有关;当作用对象为稗草时,化合物的活性可能主要与取代基R的疏水性有关.部分化合物4的抑制活性与对照药品5b,5k基本相当,但没有表现出5b,5k所具有的白化效果.化合物4与5这两类结构类似的化合物很可能在生物体内拥有不同的作用机制.
A series of non-reported 2-substituted-6-methyl-4-phenyl-3 (2H) -pyridazinones have been designed and synthesized. The structures of the compounds were confirmed by 1H NMR and elemental analysis. Ray diffraction crystal structure analysis.The bioactivity of the compounds was determined by the method of rape and pancreas and small cup of barnyardgrass.The preliminary bioassay results showed that compound 4 has good herbicidal activity.Quantitative structure-activity relationship showed that the structure of compound 4 The change of 2-position substituent in pyridazine ring affected the inhibitory activity of the compound.When the target is rape, the activity of the compound may be mainly related to the stereo parameter B4 of the substituent R and the hydrophobicity. When the target is barnyardgrass , The activity of the compound may be mainly related to the hydrophobicity of the substituent R. Part of the inhibitory activity of the compound 4 is basically the same as that of the reference drug 5b and 5k but does not show the whitening effect of 5b and 5k. Compounds with similar structure may well have different mechanisms of action in the organism.