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(Ⅱ)

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

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-羟基-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，目标化合物表现出良好的杀菌活性，其中化合物 3i 在50 mg/L时对灰霉病菌和纹枯病菌的抑制率分别为89.16%±1.73%和81.27%±1.38%，与对照药剂腐霉利（88.58%±1.64%和79.62%±1.15%）相当。初步的构效关系结果显示，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-funran were designed and synthesized. All the title compounds were characterized by IR, 1H NMR and elemental analysis. Bioassay indicated that most compounds exhibited good fungicidal activities against Botrytis cinerea,Fusarium oxysporum,Rhizoctonia solani and Corynespora cassiicola. Among them, compound 3i showed considerable fungicidal activity against B. cinerea(inhibition rate 89.16%±1.73%) and R.solani(81.27%±1.38%) at 50 mg/L, which was equal to that of the fungicide procymidone (88.58%±1.64% and 79.62%±1.15%).The preliminary structure-activity relationship indicated that the difference of R group affected the fungicidal activity.