新型氟喹啉类似物的合成、结构确定及抗真菌活性研究。
Synthesis, Structural Determination, and Antifungal Activity of Novel Fluorinated Quinoline Analogs.
机构信息
College of Biology and Environmental Engineering, Zhejiang Shuren University, Hangzhou 310015, China.
College of Chemical Engineering, Zhejiang University of Technology, Hangzhou 310014, China.
出版信息
Molecules. 2023 Apr 11;28(8):3373. doi: 10.3390/molecules28083373.
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 NMR, C NMR, and HRMS. The compound 8-fluoro-2,3-dimethylquinolin-4-yl 4-(-butyl)benzoate () was further determined by X-ray single-crystal diffraction. The antifungal activity was tested at 50 μg/mL, and the bioassay results showed that these quinoline derivatives had good antifungal activity. Among them, compounds , , , , and exhibited good activity (>80%) against , and compound displayed good activity (80.8%) against .
一系列新型氟喹啉类似物采用 Tebufloquin 作为先导化合物，以 2-氟苯胺、乙基 2-甲基乙酰乙酸酯和取代苯甲酸为原料合成。它们的结构通过 1H NMR、13C NMR 和 HRMS 得到确认。进一步通过 X 射线单晶衍射确定了化合物 8-氟-2,3-二甲基喹啉-4-基 4-(-丁基)苯甲酸酯（）。在 50 μg/mL 下测试了抗真菌活性，生物测定结果表明这些喹啉衍生物具有良好的抗真菌活性。其中，化合物 、 、 、 、 对 显示出良好的活性（>80%），化合物 对 显示出良好的活性（80.8%）。
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