Aiming to search for novel fungicide candidates,a series of novel pyrazolyl acetamides potentially targeting fungal succinate dehydrogenase(SDH)were constructed by flexibly reinventing the dualistic amide linkage that emerges in the structure of pyrazole-4-carboxamide fungicides.The diphenylether-containing pyrazole-4-acetamide(6l)featuring broad-spectrum antifungal effects was screened via a mycelium growth rate method.The above molecule exhibited the conspicuous inhibitory effect against Rhizoctonia solani,Fusarium graminearum and Botrytis cinerea at 50 μg/mL,with the inhibitory rates that were slightly better than that of hymexazol.Strikingly,the median effective concentration(EC50)of compound 6l against R.solani was estimated as 19.92 μg/mL that is better than that of hymexazol(76.74 μg/mL)and fluopyram(40.36 μg/mL).The bioactive evaluations against SDH indicated that a fungal SDH was the potential target of compound 6l for inhibiting R.solani.Subsequently,molecular docking studies implied that the diphenylether unit emerging in the structure of compound 6l could multiply interact with the pivotal residues locating at SDH protein pockets,which plays a critical role in guaranteeing the antifungal effect of diphenylether-containing pyrazole-4-acetamides.The above researches indicated that the diphenylether-containing pyrazole-4-acetamides exhibit obviously inhibitory effects against phytopathogenic fungi,and could be further optimized for developing novel fungicide candidates that could effectively control phytopathogenic fungi.
关键词
抑菌先导发现/吡唑乙酰胺/植物病原真菌/琥珀酸脱氢酶抑制剂
Key words
Discovery of antifungal lead/Pyrazolyl acetamide/Phytopathogenic fungi/Succinate dehydrogenase inhibitor
维普
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