Phytopathogenic
fungal infections have become a major threat to
agricultural production, food security, and human health globally,
and novel antifungal agents with simple chemical scaffolds and high
efficiency are needed. In this study, we designed and synthesized
38 8-hydroxyquinoline metal complexes and evaluated their antifungal
activities. The results showed that most of the tested compounds possessed
remarkable in vitro antifungal activity. Especially,
compound 1e exhibited the highest antifungal potency
among all target compounds, with EC50 values of 0.0940,
0.125, 2.95, and 5.96 μg/mL, respectively, against Sclerotinia sclerotiorum, Botrytis
cinerea, Fusarium graminearum, and Magnaporthe oryzae. Preliminary
mechanistic studies had shown that compound 1e might
cause mycelial abnormalities of S. sclerotiorum, cell membrane permeability changes, leakage of cell contents, and
inhibition of sclerotia formation and germination. Moreover, the results
of in vivo antifungal activity of compound 1e against S. sclerotiorum showed
that 1e possessed higher curative effects than that of
the positive control azoxystrobin. Therefore, compound 1e is expected to be a novel leading structure for the development
of new antifungal agents.