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目的:研究具有正丁基和取代苄基侧链结构的三唑醇类化合物的抗真菌活性。方法:设计并合成了14个1-(1H-1,2,4-三唑-1-基)-2-(2,4二氟苯基)-3-(N-正丁基-N-取代苄基氨基)-2-丙醇化合物,其结构都经过1HNMR、IR和LC-MS确证。选择8种临床常见的真菌为实验菌株,进行体外抑菌活性测试。结果:体外抑菌测试结果表明,所有化合物对除熏烟曲霉菌外的所有菌株均有一定程度的抑制活性,对深部真菌的抑制活性明显优于浅部真菌。其中化合物6a、6d和6j对石膏样小孢子菌的抑制活性(MIC800.0156μg/ml)是氟康唑的16倍;化合物6m和6n对白念珠菌的抑制活性(MIC800.0039μg/ml)是氟康唑的128倍,比其他对照药活性都高。结论:引入正丁基和取代苄基侧链的目标化合物都具有一定的抗真菌活性。
OBJECTIVE: To study the antifungal activity of triadimenol compounds with n-butyl and substituted benzyl side chains. Methods: Fourteen 1- (1H-1,2,4-triazol-1- yl) -2- (2,4-difluorophenyl) -3- Substituted benzylamino) -2-propanol compounds, all confirmed by 1H NMR, IR and LC-MS. Eight kinds of clinical common fungi were selected as experimental strains to test the antibacterial activity in vitro. Results: In vitro antibacterial test results showed that all compounds except for Aspergillus fumigatus all strains have a certain degree of inhibitory activity, the inhibitory activity of deep fungi was superior to superficial fungi. The inhibitory activity of compounds 6a, 6d and 6j against Candida gypseum (MIC800.0156μg / ml) was 16 times that of fluconazole. The inhibitory activity of compounds 6m and 6n against Candida albicans (MIC800.0039μg / ml) 128 times higher than that of the other control drugs. Conclusion: The target compounds with n-butyl and substituted benzyl side chains all have certain antifungal activity.