The ever-rising resistance in Botrytis cinerea has appeared as the awkward agricultural challenge that could be effectively resolved by developing novel fungicides featuring disparate action mechanisms. Aiming to explore novel fungicidal leads inhibiting B. cinerea, quinazolin-4(3H)-one bionic-alkaloids bearing an 1,3,4-oxadiazole fragment were conceived, synthesized, and systematically optimized under the guidance of anti-B. cinerea activities. The aforementioned optimization on molecular structures generated the anti-B. cinerea candidate I₂₅ owning the promising in vitro EC₅₀ value (0.76 μg/mL) that was fantastically superior to those of boscalid, penthiopyral, pyrimethanil and imazalil (0.86, 1.03, 15.91 and 2.15 µg/mL). Whereafter, the in vivo anti-B. cinerea preventative efficacy of an active molecule I₂₅ was noticeably evaluated as 69.3 % at 200 µg/mL, which was megascopically better than that of boscalid (60.6 %). Furthermore, the preliminary investigation on action mechanisms indicated that the fungicidal molecule I₂₅ could induce the conspicuous wrinkle on hyphal surfaces and increase the membrane permeability of B. cinerea cells. The above results have emerged as an imperative reference to developing the novel fungicides that could effectively control gray mold caused by B. cinerea.

灰葡萄孢不断上升的耐药性已成为农业面临的棘手挑战，可以通过开发具有不同作用机制的新型杀菌剂来有效解决。为了探索抑制灰霉病的新型杀菌先导化合物，在抗灰霉病的指导下，构思、合成并系统优化了带有1,3,4-恶二唑片段的喹唑啉-4(3 H )-一仿生生物碱。活动。上述分子结构优化产生了抗灰霉病候选药物I ₂₅ ，其具有良好的体外EC ₅₀值 (0.76 μg/mL)，远远优于啶酰菌胺、吡硫吡醛、嘧霉胺和抑霉唑 (0.86、1.03、15.91)。和 2.15 微克/毫升）。此后，活性分子I ₂₅的体内抗灰霉病预防功效在200μg/mL下被显着评估为69.3%，这明显优于啶酰菌胺（60.6%）。此外，作用机制的初步研究表明，杀菌分子I ₂₅可以引起菌丝表面明显的皱纹，增加灰霉病菌细胞膜的通透性。上述结果对开发能有效防治灰霉病的新型杀菌剂具有重要参考意义。