【摘 要】
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Main observation and conclusionrnIn searching for novel fungicidal leads,a series of pyrazole-containing strobilurins were rationally designed,synthesized and c
【机 构】
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State Key Laboratory of Elemento-Organic Chemistry,College of Chemistry,Nankai University,Tianjin 30
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Main observation and conclusionrnIn searching for novel fungicidal leads,a series of pyrazole-containing strobilurins were rationally designed,synthesized and charac-terized.Bioassay indicated that compound 1-7 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,1-7,displayed excellent protec-tive activity against P.sorghi.Molecular docking validated that 1-7 and azoxystrobin would share a similar binding mode with cyto-chrome bc1 complex.This study demonstrates that 1-7 is a promising fungicidal candidate for further development.
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