Synthesis, Structural Determination, and Antifungal Activity of Novel Fluorinated Quinoline Analogs

被引：5

作者：

Sun, Xinpeng ^{[1
,2
]}

Yu, Wei ^{[1
,2
]}

Min, Lijing ^{[3
]}

Han, Liang ^{[2
]}

Hua, Xuewen ^{[4
]}

Shi, Jianjun ^{[5
]}

Sun, Nabo ^{[1
]}

Liu, Xinghai ^{[2
]}

机构：

[1] Zhejiang Shuren Univ, Coll Biol & Environm Engn, Hangzhou 310015, Peoples R China

[2] Zhejiang Univ Technol, Coll Chem Engn, Hangzhou 310014, Peoples R China

[3] Huzhou Univ, Coll Life Sci, Key Lab Vector Biol & Pathogen Control Zhejiang Pr, Huzhou 313000, Peoples R China

[4] Liaocheng Univ, Coll Agr, Liaocheng 252000, Peoples R China

[5] Huangshan Univ, Coll Chem & Chem Engn, Huangshan 245041, Peoples R China

来源：

MOLECULES | 2023年 / 28卷 / 08期

关键词：

fluorinated quinoline; synthesis; antifungal activity; DERIVATIVES; DESIGN; ANTIBACTERIAL; SAR;

D O I：

10.3390/molecules28083373

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：

A series of new fluorinated quinoline analogs were synthesized using Tebufloquin as the lead compound, 2-fluoroaniline, ethyl 2-methylacetoacetate, and substituted benzoic acid as raw materials. Their structures were confirmed by H-1 NMR, C-13 NMR, and HRMS. The compound 8-fluoro-2,3-dimethylquinolin-4-yl 4-(tert-butyl)benzoate (2b) was further determined by X-ray single-crystal diffraction. The antifungal activity was tested at 50 mu g/mL, and the bioassay results showed that these quinoline derivatives had good antifungal activity. Among them, compounds 2b, 2e, 2f, 2k, and 2n exhibited good activity (>80%) against S. sclerotiorum, and compound 2g displayed good activity (80.8%) against R. solani.

引用

页数：10

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