College of Pharmacy, Guizhou Provincial Engineering Technology Research Center for Chemical Drug R&D, Guizhou Provincial Key Laboratory of Pathogenesis and Drug Research on Common Chronic Diseases, Guizhou Medical University, Guiyang, People's Republic of China.
Nat Prod Res. 2024 Jul;38(14):2441-2446. doi: 10.1080/14786419.2023.2177993. Epub 2023 Feb 10.
Phthalide, benzoxazole, and chromene are important heterocyclic skeletons with extensive biological activities. In order to develop novel potential antifungal agents, twenty-two benzoxazole/chromene-containing phthalide derivatives were prepared, and their fungicidal activity against nine common plants pathogenic fungi were evaluated . The EC values indicated that compound displayed superior antifungal activity against e (11.0 g/mL), (8.5 g/mL), (27.8 g/mL), (3.1 g/mL) and (4.3 g/mL) strains, which was more potent than the two commercialized fungicides hymexazol and chlorothalonil. In addition, the structure-activity relationship analysis demonstrated that the combination site of oxazolamide with phthalide has an important effect on antifungal activity. This research offers a potential compound for the development of novel agricultural fungicides.
苯并恶唑、色烯是含重要杂环骨架，具有广泛的生物活性。为了开发新型潜在的抗真菌剂，合成了 22 个苯并恶唑/色烯基苯酞衍生物，并评价了它们对 9 种常见植物病原真菌的杀菌活性。EC 值表明，化合物 对 e（11.0μg/mL）、 （8.5μg/mL）、 （27.8μg/mL）、 （3.1μg/mL）和 （4.3μg/mL）菌株表现出优异的抗真菌活性，比两种商品化杀菌剂 hymexazol 和 chlorothalonil 的活性更强。此外，构效关系分析表明，苯并恶唑酰胺与苯酞的结合部位对其杀菌活性有重要影响。该研究为新型农用杀菌剂的开发提供了一种潜在的化合物。
