崔紫宁, 梁志彬, 田芳, 刘诗胤, 闫晓静. 含5-苯基2-呋喃环的3(2H)哒嗪酮类衍生物的合成与生物活性(I)[J]. 农药学学报, 2014, 16(3): 252-258. DOI: 10.3969/j.issn.1008-7303.2014.03.03
    引用本文: 崔紫宁, 梁志彬, 田芳, 刘诗胤, 闫晓静. 含5-苯基2-呋喃环的3(2H)哒嗪酮类衍生物的合成与生物活性(I)[J]. 农药学学报, 2014, 16(3): 252-258. DOI: 10.3969/j.issn.1008-7303.2014.03.03
    CUI Zining, LIANG Zhibin, TIAN Fang, LIU Shiyin, YAN Xiaojing. Synthesis and bioactivity of novel pyridazin-3(2H)-one derivatives containing 5-phenyl-2-furan (I)[J]. Chinese Journal of Pesticide Science, 2014, 16(3): 252-258. DOI: 10.3969/j.issn.1008-7303.2014.03.03
    Citation: CUI Zining, LIANG Zhibin, TIAN Fang, LIU Shiyin, YAN Xiaojing. Synthesis and bioactivity of novel pyridazin-3(2H)-one derivatives containing 5-phenyl-2-furan (I)[J]. Chinese Journal of Pesticide Science, 2014, 16(3): 252-258. DOI: 10.3969/j.issn.1008-7303.2014.03.03

    含5-苯基2-呋喃环的3(2H)哒嗪酮类衍生物的合成与生物活性(I)

    Synthesis and bioactivity of novel pyridazin-3(2H)-one derivatives containing 5-phenyl-2-furan (I)

    • 摘要: 为探索新的农药先导化合物,经取代苯基呋喃甲酰氯与5-肼基-3(2H)哒嗪酮反应,得到15个未见文献报道的含呋喃环3(2H)哒嗪酮类化合物,其结构均通过了红外光谱、核磁共振氢谱和元素分析确认。初步生物活性测定结果表明,目标化合物具有良好的杀菌活性,但杀虫活性较弱。其中化合物 3k 在50 mg/L时对灰霉病菌的抑制率为86.29%±1.51%,与对照药剂腐霉利相当。初步的构效关系研究结果显示,苯环上取代基的种类和位置对杀菌活性有重要影响。

       

      Abstract: A series of novel pyridazin-3(2H)-one derivative with 5-phenyl-2-furan were designed and synthesized. All the title compounds were characterized by IR, 1H NMR and elemental analysis. Bioassay indicated that the title compounds had low insecticidal effects on Plutella xylostella, Mythimna separate and Culex pipiens pallens, but most compounds exhibited good fungicidal activities against Botrytis cinerea, Fusarium oxysporum and Corynespora cassiicola. In particular, compounds 3 k showed considerable activity (86.29%±1.51%) against B. cinerea at 50 mg/L, which was equal to the fungicide procymidone. The preliminary structure-activity relationship showed that the difference of R group affected the fungicidal activity.

       

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