设计、合成及 6-取代基 3-正丁基苯酞衍生物对植物病原真菌的抗真菌活性。
Design, Synthesis and Antifungal Activities of 6-Substituted 3-Butylphthalide Derivatives against Phytopathogenic Fungi.
机构信息
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.
出版信息
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。
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