Design, Synthesis and Antifungal Activities of 6-Substituted 3-Butylphthalide Derivatives against Phytopathogenic Fungi

被引：16

作者：

Li, Yong ^{[1
]}

Luo, Zhongfu ^{[1
]}

Luo, Bilan ^{[1
]}

Lan, Qing ^{[1
]}

Fan, Judi ^{[1
]}

Xue, Wei ^{[2
]}

Miao, Jing ^{[1
]}

Li, Yi ^{[1
]}

Tang, Lei ^{[1
]}

Fan, Lingling ^{[1
]}

机构：

[1] Guizhou Med Univ, State Key Lab Funct & Applicat Med Plants, Guizhou Prov Engn Technol Res Ctr Chem Drug R&D, Coll Pharm, Guiyang 550004, Peoples R China

[2] Guizhou Univ, Key Lab Green Pesticide & Agr Bioengn, Minist Educ, Guiyang 550025, Peoples R China

来源：

CHEMISTRY & BIODIVERSITY | 2020年 / 17卷 / 10期

关键词：

butylphthalide derivatives; antifungal activity; phytopathogenic fungi; synthesis; CNIDIUM-OFFICINALE; Z-LIGUSTILIDE; ANTIBACTERIAL; SINENSIS;

D O I：

10.1002/cbdv.202000435

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

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 mu g/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(50)of 3-butyl-6-nitro-2-benzofuran-1(3H)-one against FS, FO and FG were 6.6, 9.6 and 16.0 mu g/mL, respectively. The EC(50)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 mu g/mL, respectively. The preliminary structure-activity relationships (SARs) of all target compounds were also investigated.

引用

页数：9

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