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目的合成一系列8-氟-2,3-二氢喹啉-4(1H)-酮缩氨基脲类化合物,测定其体外抗真菌活性。方法以邻氟苯胺为起始原料,经与丙烯酸加成、在多聚磷酸(PPA)中环合制得中间体8-氟-2,3-二氢喹啉-4(1H)-酮;该中间体与各种N4-取代的氨基脲缩合得到目标化合物。采用二倍浓度稀释法测试各目标化合物的体外抗真菌活性,实验选用8种临床上常用的致病真菌为测试菌株,以氟康唑、伊曲康唑为阳性对照药。结果与结论16个8-氟-2,3-二氢喹啉-4(1H)-酮缩氨基脲类化合物均未见文献报道,其结构经1H-NMR、MS谱确证;活性测试结果表明,合成的多个目标化合物对测试真菌表现出较好的体外抑菌活性,尤其是对红色毛藓菌的活性均好于阳性对照药。
Aim To synthesize a series of 8-fluoro-2,3-dihydroquinolin-4 (1H) -one semicarbazones and determine their antifungal activity in vitro. Methods The o-fluoroaniline was used as the starting material to synthesize 8-fluoro-2,3-dihydroquinolin-4 (1H) -one by cyclization in polyphosphoric acid (PPA) The intermediate is condensed with various N4-substituted semicarbazide to give the title compound. In vitro antifungal activity of each compound was tested by double dilution method. Eight kinds of clinically used pathogenic fungi were selected as test strains and fluconazole and itraconazole as positive control. Results and Conclusions None of the 16 8-fluoro-2,3-dihydroquinolin-4 (1H) -one semicarbazones have been reported in the literature. Their structures were confirmed by 1H-NMR and MS spectra. The results of the activity test . The synthesized target compounds showed good antibacterial activities in vitro against the tested fungi, especially against Tricholoma grossedentum.