新型含芳基吡唑的3(2<i>H</i>)-哒嗪酮衍生物的设计、合成及杀菌活性

新型含芳基吡唑的3(2H)-哒嗪酮衍生物的设计、合成及杀菌活性

摘要: 为了寻找高活性杀菌化合物，采用中间体衍生化法将哒嗪酮结构单元引入到芳基吡唑中间体中，设计并合成了一系列结构新颖的化合物C1~C22，其结构经核磁共振氢谱(¹H NMR)、碳谱(¹³C NMR)、高分辨质谱(HRMS)确证。通过先导发现、结构优化，发现在苯环4位引入F原子使得该类化合物活性表现更优(化合物C14)，其在6.25 mg/L剂量下对黄瓜霜霉病防效为100%，明显优于对照药剂氟吗啉(防效为10%)；在更低剂量3.13 mg/L下对黄瓜霜霉病的防效为85%，与对照药剂氰霜唑防效相当(85%)，值得进一步研究。

Abstract: In order to discover the compounds with high fungicidal activities, a series of novel compounds(C1-C22) were designed and synthesized by synthesised using the Intermediate Derivatisation Method (IDM). The arylpyrazole intermediate was modified by introducing a pyridazine substructure, and the resulting compounds were characterized by ¹H NMR, ¹³C NMR and HRMS. By means of the lead discovery and structural optimization, the compound C14 bearing 4-F atom in the benzene ring with optimal activity was found, which showed significantly better activity(100%) than the control compound flumorph(10%) at 6.25 mg/L against cucumber downy mildew, and equal control efficacy at a lower dose of 3.13 mg/L (85% control efficacy) to the commercial cyazofamid(85% control efficacy). Further research is warranted.