新型二苯胺衍生物的设计、合成及构效关系
Design, synthesis and structure-activity relationship of novel diphenylamine derivatives.
作者信息
Li Huichao, Guan Aiying, Huang Guang, Liu Chang-Ling, Li Zhinian, Xie Yong, Lan Jie
机构信息
State Key Laboratory of the Discovery and Development of Novel Pesticide, Shenyang Research Institute of Chemical Industry Co. Ltd, Shenyang 110021, China.
State Key Laboratory of the Discovery and Development of Novel Pesticide, Shenyang Research Institute of Chemical Industry Co. Ltd, Shenyang 110021, China.
出版信息
Bioorg Med Chem. 2016 Feb 1;24(3):453-61. doi: 10.1016/j.bmc.2015.09.032. Epub 2015 Sep 21.
Diphenylamine derivatives have been reported with good fungicidal, insecticidal, acaricidal, rodenticidal and/or herbicidal activities. To find new lead compound of this kind, a series of novel diphenylamine derivatives were designed and synthesized by the approach of Intermediate Derivatization Methods. All compounds were identified by (1)H NMR and elemental analysis. Bioassays demonstrated that some compounds substituted at 2,4,6-positions or 2,4,5-positions of phenyl ring B exhibited excellent fungicidal activities. The optimal compounds P30 and P33 showed 80% and 85% control respectively against cucumber downy mildew at 12.5mgL(-1), both 100% control against rice blast at 0.3mgL(-1) and both 100% control against cucumber gray mold at 0.9mgL(-1). The relationship between structure and fungicidal activities was discussed as well.
据报道，二苯胺衍生物具有良好的杀菌、杀虫、杀螨、杀鼠和/或除草活性。为了寻找此类新的先导化合物，通过中间体衍生化方法设计并合成了一系列新型二苯胺衍生物。所有化合物均通过¹H NMR和元素分析进行鉴定。生物测定表明，一些在苯环B的2,4,6-位或2,4,5-位被取代的化合物表现出优异的杀菌活性。最优化合物P30和P33在12.5mgL⁻¹时对黄瓜霜霉病的防治率分别为80%和85%，在0.3mgL⁻¹时对稻瘟病的防治率均为100%，在0.9mgL⁻¹时对黄瓜灰霉病的防治率均为100%。同时还讨论了结构与杀菌活性之间的关系。
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