Design, Synthesis, and Antifungal Evaluation of Novel Quinoline Derivatives Inspired from Natural Quinine Alkaloids.

Inspired by quinine and its analogues, we designed, synthesized, and evaluated two series of quinoline small molecular compounds ( and ) and six series of quinoline derivatives (-) for their antifungal activities. The results showed that compounds and series exhibited significant fungicidal activities. Significantly, compounds (EC = 0.41 μg/mL) and (EC = 0.55 μg/mL) displayed the superior in vitro fungicidal activity and the potent in vivo curative effect against . Preliminary mechanism studies showed that compounds and could cause changes in the cell membrane permeability, accumulation of reactive oxygen species, loss of mitochondrial membrane potential, and effective inhibition of germination and formation of sclerotia. These results indicate that compounds and are novel potential fungicidal candidates against derived from natural products.