To reduce the harm of agriculture production and ecological environment by Rhizoctonia solani AG-1-IB, it is urgent to develop new fungicidal with better selectivity. Cyanuric chloride has the unique physical, chemical and biological activity, after it reacted with aliphatic amino and aromatic amino via nucleophilic substitution, 1,3,5-triazine derivatives containing amino groups were obtained. Based on the principles of bioisosterism and bioactive substructure combination, the bioactive heterocyclic groups of 1,3, 5-triazine derivatives containing amino moiety were introduced into the isoxazole ring of the fungicidal hymexazol. Four novel 1,3,5-triazine derivatives including isoxazole ring were designed and synthesized . The four target moleculars were confirmed by H-nuclear magnetic resonance and mass spectra. The preliminary bioassay by plate method shows that the four target compouds have better fungicidal activity against Rhizoctonia solani AG-1-IB; at a concentration of 200 μg · mL-1, 1,3,5-triazine derivatives 4b and 4c are efftective to inhabit Rhizoctonia solani AG-1-IB.%为了减少草坪褐斑病菌对农业生产和生态环境造成的损失,急需要开发选择性好的新型杀菌剂.三聚氯氰具有独特的物理化学和生物活性,与脂肪胺、芳香胺亲核取代反应后,生成胺基取代-1,3,5-三嗪类衍生物.根据生物电子等排和生物活性亚结构拼接原理,将氨基取代-1,3,5-三嗪类杂环化合物的结构引入到杀菌剂恶霉灵的异恶唑环中,设计并合成了4个结构新颖的含有异恶唑环的1,3,5-三嗪类衍生物,其结构经核磁共振氢谱和质谱确认.通过平皿法进行初步生物活性测试,4个目标化合物均对草坪褐斑病菌具有较好的杀菌活性,其中化合物4b,4c在质量浓度为200 μg·mL-1时能够有效抑制草坪褐斑病菌.
展开▼
