The ever-rising resistance in 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 , quinazolin-4(3)-one bionic-alkaloids bearing an 1,3,4-oxadiazole fragment were conceived, synthesized, and systematically optimized under the guidance of anti- activities. The aforementioned optimization on molecular structures generated the anti- candidate owning the promising EC 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 anti- preventative efficacy of an active molecule 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 could induce the conspicuous wrinkle on hyphal surfaces and increase the membrane permeability of cells. The above results have emerged as an imperative reference to developing the novel fungicides that could effectively control gray mold caused by .

中文翻译：

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带有 1,3,4-恶二唑片段的新型喹唑啉-4(3H)-一仿生生物碱作为抑制灰葡萄孢的潜在杀菌剂：设计、合成和生物活性引导的结构优化


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。为了探索新型杀菌先导化合物，在抗活性的指导下，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)-一仿生生物碱。上述分子结构的优化产生了具有有前景的 EC 值 (0.76 µg/mL) 的抗候选药物，该值远远优于啶酰菌胺、吡噻醛、嘧霉胺和抑霉唑 (0.86、1.03、15.91 和 2.15 µg/mL)。此后，活性分子的抗预防功效在 200 µg/mL 时显着评估为 69.3%，明显优于啶酰菌胺 (60.6%)。此外，作用机制的初步研究表明，该杀菌分子可以引起菌丝表面明显的皱纹，增加细胞膜的通透性。上述结果对开发有效防治灰霉病的新型杀菌剂具有重要参考意义。