【作者】 王奎； 康晶欣； 叶非； 付颖；

【Author】 Ying Fu;Kui Wang;Jing-Xin Kang;Fei Ye;College of Science, Northeast Agricultural University;

【机构】 东北农业大学理学院；

【摘要】 [目的]新型高效4-羟基苯丙酮酸双加氧酶（HPPD）抑制剂的设计合成、生物活性和构效关系研究。[方法]以吡唑特为模板化合物,利用生物电子等排原理进行结构修饰,设计合成了23个芳基萘甲酮类化合物。所合成的化合物采用FTIR、¹H NMR、¹³CNMR和HRMS对其结构进行表征。[结果]本文合成的23个芳基萘甲酮类化合物在3 kg/ha剂量下茎叶处理具有良好的除草活性,其中化合物3h显示出最高的除草活性。[结论]芳基萘甲酮类化合物可作为新型HPPD抑制剂的先导化合物。更多还原

【Abstract】 [Aims]In an attempt to search for novel 4-hydroxyphenylpyruvate dioxygenase（HPPD）inhibitors with highly herbicidal active.[Methods]The commercial herbicide Pyrazolynate was modified by the bioisostere principle,and the structure was characterized by ¹ H NMR and ¹³C NMR.[Results]The 23 aryl-naphthyl methanone compounds were synthesized and reported for the first time.The bioassay studies indicated some of these derivatives exhibited preferable herbicidal activity at the rate of 3 kg/ha by post-emergence application,in which compound 3 e displayed the best herbicidal activity.[Conclusions]Aryl-naphthyl methanone motif could be a potential lead structure for further development of novel herbicides.更多还原