新型酰胺类化合物的合成及抗植物病原真菌活性研究

Synthesis and screening for potential against phytopathogenic fungi activity of novel amides

为了寻找具有潜在抗真菌活性的新型农用化学品,我们以瑞香狼毒中提取的二苯酮类似物为先导,设计并合成了一系列的酰胺类化合物,并进行了以下5种植物真菌的筛选:水稻纹枯病菌(Rhizoctonia solani)、小麦赤霉病菌(Gibberella zeae)、玉米小斑病菌(Bipolarismaydis)、番茄灰霉病菌(Botrytis cirerea)和油菜菌核病菌(Sclerotinia sclerotiorum).初步的活性筛选研究显示:氮-(2-氟苯基)-2,4,5-三甲基-3-呋喃甲酰胺(p)具有很强的抗水稻纹枯病菌活性(在20和200 mg/L的浓度下抑制率分别为98%和99%);氮-(4-氟苯基)-2,5-二甲基-3-呋喃甲酰胺(h)和氮-(2-氟苯基)-2,5-二甲基-3-呋喃甲酰胺(k)这两种化合物在200 mg/L浓度下对油菜菌核病菌的抑制率分别为94%和90%.病原真菌毒力测试表明,化合物k的EC_(50)值为0.034 mg/L,优于作为参考的多菌灵(0.050 mg/L).根据化合物k的抑菌活性和EC_(50)结果,我们可以推断化合物k对水稻纹枯病菌具有很好的抑制活性.因此,化合物k被证明是最具深入研究潜力的化合物.

In order to search for novel agrochemicals with potential anti-phythopathogenic fungi activity, a series of daphneone analogues were designed and synthesized. They were screened for antifungal activi- ties against five phytopathogenic fungi： Rhizoctonia solani , Botrytis cirerea , Gibberella zeae , Bipolaris maydis, and Sclerotia sclerotium. The preliminary bioassays indicated that some compounds exhibited a fairly good activity. N-（2-fluorophenyl）-2, 4, 5-trimethyl-3-furancarboxamide （p） showed a strong fungistatic activity against R. solani （98% and 99% growth inhibition at 20 and 200 mg/L, respectively）. Two compounds, N-（4-fluorophenyl）-2, 5-dimethyl-3-furanearboxamide （h） and N- （2-fluorophenyl）-2, 5-dimethyl-3-furanearboxamide （k） at 200 mg/L inhibited the growth of Sclerotia sclerotium at 94% and 90~~, respectively. The ECs0 values for compound k were 0. 034 rag/L, while for the control fungicide earbendazim were 0.050 mg/L. According to the EC50 and the preventive activity of compound k, it can be inferred that compound k had a very good activity against Rhizoctonia solani. Thus, the compound k was demonstrated to be the most promising candidate for further study.