In searching for novel fungicidal leads, a series of pyrazole-containing strobilurins were rationally designed, synthesized and characterized. Bioassay indicated that compound I-7 displayed excellent fungicidal activity against a broad spectrum of plant pathogens such as Gibberella zeae, Rhizoctonia cerealis, Sclerotinia sclerotiorum, Phytophthora infestans, Physalospora piricola and Pellicularia sasakii with EC₅₀ of 0.16, 0.02, 0.72, 0.07, 0.77 and 0.65 μg/mL, respectively, which were 3—10 times more potent than the positive control azoxystrobin against the corresponding pathogens. Moreover, like azoxystrobin and kresoxim methyl, I-7, displayed excellent protective activity against P. sorghi. Molecular docking validated that I-7 and azoxystrobin would share a similar binding mode with cytochrome bc₁ complex. This study demonstrates that I-7 is a promising fungicidal candidate for further development.

中文翻译：

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新型含吡唑的Strobilurin衍生物的设计，合成和杀真菌活性评估†

在寻找新颖的杀真菌线索时，合理设计，合成和表征了一系列含吡唑的球蛋白。生物测定表明，化合物I-7对多种植物病原菌（如赤霉菌，谷物根瘤菌，菌核盘菌，致病疫霉，皮氏假单胞菌和Sasakii菌）表现出优异的杀真菌活性，EC ₅₀为0.16，0.02，0.72，0.07，浓度分别为0.65μg/ mL和0.65μg/ mL，比抗相应病原体的阳性对照嘧菌酯的效力高3-10倍。此外，I-7像嘧菌酯和克雷索辛甲基一样，对高粱假单胞菌也显示出优异的保护活性。。分子对接验证了I-7和嘧菌酯将与细胞色素bc ₁复合物共享相似的结合模式。这项研究表明I-7是有希望的杀真菌剂，可用于进一步开发。