| Summary: | A series of 30 succinate dehydrogenase inhibitors (SDHIs) of 4-amino coumarin-based derivatives were designed and synthesized. According to the analysis of fungicidal activity in vitro, most of the compounds expressed broad-spectrum antifungal activity against four plant pathogenic fungi (<i>Alternaria alternata, Alternaria solani, Fusarium oxysporum,</i> and <i>Botrytis cinerea</i>) using the mycelium growth inhibition method. The results showed that compounds <b>3n</b> with the group of 2-ene-3-methyl-butyl and <b>4e</b> with the group of 2-bromo-1-oxo-hexyl displayed excellent activity against <i>Alternaria alternata</i> and <i>Alternaria solani</i>, with EC<sub>50</sub> values of 92~145 μg/mL. Molecular docking showed that the inhibitor <b>3n</b> was completely locked into the cavity of SDH, forming a conventional hydrogen bond interacting with the amino acid residue TYR58. The present work indicates that these derivatives would serve as novel potential fungicides targeting SDH.
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