State Key Laboratory of Functions and Applications of Medicinal Plants, College of Pharmacy, Guizhou Provincial Engineering Technology Research Center for Chemical Drug R&D, Guizhou Medical University, Guiyang, 550004, P. R. China.
Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Guizhou University, Guiyang, 550025, P. R. China.
Chem Biodivers. 2020 Oct;17(10):e2000435. doi: 10.1002/cbdv.202000435. Epub 2020 Sep 21.
In order to discover novel potential antifungal agents, a series of 6-substituted 3-butylphthalide derivatives were designed, synthesized and evaluated for their antifungal activities against nine phytopathogenic fungi. Preliminary bioassay tests showed that five 3-butylphthalide derivatives exhibited more potent antifungal activities than hymexazol at the concentration of 50 μg/mL. Especially, 3-butyl-6-nitro-2-benzofuran-1(3H)-one and 3-butyl-6-hydroxy-5-nitro-2-benzofuran-1(3H)-one had significant fungicidal activity against some phytopathogenic fungi. The EC of 3-butyl-6-nitro-2-benzofuran-1(3H)-one against FS, FO and FG were 6.6, 9.6 and 16.0 μg/mL, respectively. The EC of 3-butyl-6-hydroxy-5-nitro-2-benzofuran-1(3H)-one against BC, PO, VM, SS and AS were 6.3, 5.9, 10.0, 4.5 and 8.4 μg/mL, respectively. The preliminary structure-activity relationships (SARs) of all target compounds were also investigated.
为了发现新的潜在抗真菌剂，设计、合成了一系列 6-取代 3-丁基苯酞衍生物，并评估了它们对 9 种植物病原菌的抗真菌活性。初步生物测定试验表明，在 50μg/mL 的浓度下，有 5 种 3-丁基苯酞衍生物比 hymexazol 具有更强的抗真菌活性。特别是 3-丁基-6-硝基-2-苯并呋喃-1(3H)-酮和 3-丁基-6-羟基-5-硝基-2-苯并呋喃-1(3H)-酮对一些植物病原菌具有显著的杀菌活性。3-丁基-6-硝基-2-苯并呋喃-1(3H)-酮对 FS、FO 和 FG 的 EC 分别为 6.6、9.6 和 16.0μg/mL。3-丁基-6-羟基-5-硝基-2-苯并呋喃-1(3H)-酮对 BC、PO、VM、SS 和 AS 的 EC 分别为 6.3、5.9、10.0、4.5 和 8.4μg/mL。还对所有目标化合物的初步构效关系(SARs)进行了研究。
