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Synthesis, Structural Determination, and Antifungal Activity of Novel Fluorinated Quinoline Analogs
oleh: Xinpeng Sun, Wei Yu, Lijing Min, Liang Han, Xuewen Hua, Jianjun Shi, Nabo Sun, Xinghai Liu
| Format: | Article |
|---|---|
| Diterbitkan: | MDPI AG 2023-04-01 |
Deskripsi
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 <sup>1</sup>H NMR, <sup>13</sup>C NMR, and HRMS. The compound 8-fluoro-2,3-dimethylquinolin-4-yl 4-(<i>tert</i>-butyl)benzoate (<b>2b</b>) 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 <b>2b</b>, <b>2e</b>, <b>2f</b>, <b>2k</b>, and <b>2n</b> exhibited good activity (>80%) against <i>S. sclerotiorum</i>, and compound <b>2g</b> displayed good activity (80.8%) against <i>R. solani</i>.