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.
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收藏
页数:10
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