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目的基于喹啉类和噻吩类抗真菌化合物的构效关系,设计合成含喹啉和噻吩结构片段的新型抗真菌化合物,并测试其对白念珠菌的抑制活性。方法以5-氰基噻吩-2-甲醛或者5-氰基噻吩-3-甲醛为起始原料,经还原氨化、氰基还原、与喹啉甲酸或异喹啉甲酸的酰胺化等反应,合成13个目标化合物,并通过1 H NMR和MS确证其化学结构,以微量液基稀释法测定这些化合物体外抗白念珠菌SC5314活性。结果目标化合物均具有一定的抗真菌活性,其中化合物6k显示很好的抗真菌活性,MIC80值为0.5μg/ml,与对照药氟康唑相当。结论所设计合成的含喹啉和噻吩结构片段的新型化合物具有较好的体外抗真菌活性,值得深入研究。
OBJECTIVE Based on the structure-activity relationship of quinolines and thiophene antifungal compounds, a novel antifungal compound containing quinoline and thiophene structural fragments was designed and tested for its inhibitory activity against Candida albicans. Methods Starting from 5-cyanothiophene-2-carbaldehyde or 5-cyanothiophene-3-carbaldehyde, the compound was reductively aminated, reduced with cyano, reacted with quinolinecarboxylic acid or isoquinolinecarboxylic acid, Thirteen compounds were synthesized and their chemical structures were confirmed by 1 H NMR and MS. The activity of these compounds against Candida albicans SC5314 was determined in vitro by micro fluid-based dilution. Results The target compounds all had certain antifungal activity. Compound 6k showed good antifungal activity with a MIC80 value of 0.5 μg / ml, comparable to the control drug fluconazole. Conclusion The novel compounds containing quinoline and thiophene structures designed and synthesized have good antifungal activity in vitro and deserve further study.