苯并三唑 - 偶氮 - 苯酚/苯胺衍生物作为抗真菌剂的发现。
Discovery of benzotriazole-azo-phenol/aniline derivatives as antifungal agents.
作者信息
Lv Min, Ma Jingchun, Li Qin, Xu Hui
机构信息
Research Institute of Pesticidal Design & Synthesis, College of Plant Protection, Northwest A&F University, Yangling 712100, Shaanxi Province, China.
Research Institute of Pesticidal Design & Synthesis, College of Plant Protection, Northwest A&F University, Yangling 712100, Shaanxi Province, China; Shaanxi Key Laboratory of Natural Products & Chemical Biology, College of Chemistry and Pharmacy, Northwest A&F University, Yangling 712100, Shaanxi Province, China.
出版信息
Bioorg Med Chem Lett. 2018 Jan 15;28(2):181-187. doi: 10.1016/j.bmcl.2017.11.032. Epub 2017 Nov 16.
A series of benzotriazole-azo-phenol/aniline derivatives were prepared and evaluated for their antifungal activities against six phytopathogenic fungi such as Fusarium graminearum, Fusarium solani, Alternaria alternate, Valsa mali, Botrytis cinerea, and Curvularia lunata. Among them, compounds IIf, IIn, and IIr showed a broad-spectrum of potent antifungal activities. Especially some compounds displayed 3.5-10.8 folds more potent activities than carbendazim against A. alternata and C. lunata. Notably, compounds IIc, IIm, and IIr exhibited good protective and therapeutic effects against B. cinerea at 200 μg/mL. Their structure-activity relationships were also discussed.
制备了一系列苯并三唑 - 偶氮 - 苯酚/苯胺衍生物，并对其针对六种植物病原真菌（如禾谷镰刀菌、茄腐镰刀菌、链格孢、苹果黑腐皮壳菌、灰葡萄孢和新月弯孢菌）的抗真菌活性进行了评估。其中，化合物IIf、IIn和IIr表现出广谱的强效抗真菌活性。特别是一些化合物对链格孢和新月弯孢菌的活性比多菌灵高3.5 - 10.8倍。值得注意的是，化合物IIc、IIm和IIr在200μg/mL时对灰葡萄孢表现出良好的保护和治疗效果。还讨论了它们的构效关系。
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