Design, Synthesis and Antifungal Activity of Novel 1,4-Pentadiene-3-one Containing Quinazolinone.

Twenty 1,4-pentadiene-3-one derivatives containing quinazolinone (-) were designed and synthesized. The bioactivity test results showed that some compounds had antifungal activities in vitro. showed excellent bioactivity against () and sp., with EC values of 0.70 and 3.84 μg/mL, which are higher than those of the control drug azoxystrobin at 8.15 and 17.25 μg/mL. In vivo activity tests were carried out on oilseed rape and kiwifruit. The protective effect of on oilseed rape infected with (91.7 and 87.3%) was better than that of azoxystrobin (90.2 and 79.8%) at 100 and 50 μg/mL, respectively, and the protective effect on kiwifruit infected with sp. (96.2%) was better than that of azoxystrobin (94.6%) at 200 μg/mL. Scanning electron microscopy results showed the hyphae of treated with compound abnormally collapsed and shriveled, inhibiting the growth of mycelium and, thus, laying the inhibiting effect on . The results of the mechanism research showed that the action of changed the mycelial morphology of , affected the permeability of cells, increased the leakage of cytoplasm and allowed the cell membrane to break down. This study shows that 1,4-pentadiene-3-one derivatives containing quinazolinone have good effects on plant fungi and the potential for becoming new fungicides.