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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。
In order to explore a new pesticide lead compound, 15 novel pyridazinones containing furan ring 3 (2H) were obtained by reaction of substituted phenyl furoyl chloride with 5-hydroxy-3 (2H) pyridazinone. Its structure has passed the infrared spectroscopy, 1H nuclear magnetic resonance and elemental analysis confirmed. The preliminary bioassay results showed that the target compounds showed good bactericidal activity. The inhibitory rates of compound 3i against Botrytis cinerea and Rhizoctonia solani were 89.16% ± 1.73% and 81.27% ± 1.38% at 50 mg / L, respectively. , Comparable to that of the control medicament (88.58% ± 1.64% and 79.62% ± 1.15%). The preliminary structure-activity relationship results show that the types and positions of substituents on the benzene ring have an important influence on the bactericidal activity.