新型三唑类衍生物的合成及抗真菌活性研究  

Synthesis and antifungal activities of novel triazole derivatives

作　　者：汤淏[1] 黄鲁[1] 张治强[2] 苏华[1] 吴茂诚[2] 任海祥[1] 王曙东[1] 

机构地区：[1]南京军区南京总医院制剂科,南京210002 [2]第二军医大学药学院有机化学教研室,上海200433

出　　处：《药学服务与研究》2015年第2期111-114,共4页Pharmaceutical Care and Research

基　　金：国家自然科学基金(20972188)

摘　　要：目的:研究具有萘苄结构的三唑类化合物的抗真菌活性。方法:设计合成了10个三唑类新化合物,其结构通过1 H-NMR、MS确证,选择8种真菌为实验菌株,进行体外抑菌活性测试。结果:所有化合物对所选真菌均表现出了一定的抑菌活性,部分化合物对白念珠菌的MIC80值<0.125μg/ml,是伏立康唑活性的16倍。结论:引入萘环和烷基侧链的目标化合物都具有抗真菌活性。Objective：To synthesize a new series of triazole compounds with naphthalene benzyl side chain and evaluate their antifungal activities.Methods：Ten compounds were synthesized and identified by 1 H-NMR,MS spectra.The in vitro antifungal activities of all the compounds were evaluated against eight human pathogenic fungi.Results：All of the compounds exhibited potent antifungal activities,some compounds showed high activities against Candida albicans with the MIC80 values of less than 0.125μg/ml,which was 16 times higher than that of voriconazole.Conclusion：The target compounds with naphthalene and alkane substituents showed potent antifungal activities.

关 键 词：三唑类衍生物 化学合成 抗真菌活性 

分 类 号：R914.5[医药卫生—药物化学] R978.5[医药卫生—药学]