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目的:研究不同取代哌嗪侧链的引入对三唑醇类化合物抗真菌活性的影响。方法:设计合成了11个三唑醇类新化合物;选择8种真菌(白色念珠菌,新生隐球菌,热带念珠菌,近平滑念珠菌,红色毛癣菌,羊毛状小孢子菌,紧密着色真菌及薰烟曲霉菌)为实验菌株,进行体外抑菌活性测试。结果:目标化合物对8种真菌特别是深部真菌均有一定的抑制活性,其中有7个化合物对白念珠菌的MIC80值≤0.125μg/ml,是氟康唑活性的4倍以上,与伊曲康唑活性相当。结论:脂水分配系数和立体化学因素的改变对该类化合物体外抑菌活性有较大影响。
Objective: To study the effect of different substituted piperazine side chains on the antifungal activity of triadimenol. Methods: Eleven new triazole compounds were designed and synthesized. Eight kinds of fungi (Candida albicans, Cryptococcus neoformans, Candida tropicalis, Candida parapsilosis, Trichophyton rubrum, Microsporum lanuginosa, And Aspergillus fumigatus) as experimental strains, in vitro antibacterial activity test. Results: The target compounds had certain inhibitory activity against eight fungi, especially deep fungi. Among them, seven compounds had a MIC80 value of 0.125 μg / ml against Candida albicans, more than four times higher than that of fluconazole, The activity of azole is comparable. Conclusion: The change of lipids partition coefficient and stereochemical factors have a great influence on the antibacterial activities of these compounds in vitro.