Synthesis and biological evaluation of novel triazole derivatives as antifungal agents

作     者：Hui Tang Can-Hui Zheng Xiao-Hui Ren Jia Liu Na Liu Jia-Guo Lv Ju Zhu You-Jun Zhou 

作者机构：PharmacyProvincial Hospital Affiliated to Shandong University School of PharmacySecond Military Medical University 

出 版 物：《Chinese Chemical Letters》 (中国化学快报（英文版）)

年 卷 期：2013年第24卷第3期

页      面：219-222页

核心收录：

学科分类：1007[医学-药学(可授医学、理学学位)] 100705[医学-微生物与生化药学] 10[医学] 

基　　金：supported by the National Natural Science Foundation of China(Nos.20972187 and 30901859) Shanghai Natural Science Foundation(No.09ZR1438800) Shandong Natural Science Foundation(No.ZR2012HQ026) 

主　　题：TriazoleAntifungalStructure activity relationshipCYP51 

摘      要：A series of 1-（benzylamino）-2-（2,4-difiuorophenyl）-3-（lH-1,2,4-triazol-l-yl）propan-2-ols compounds were synthesized and evaluated for their antifungal activities in vitro. The results showed that compounds 6A and 6B exhibited good antifungal activity. Compound 6tt8 showed the strongest antifungal activity, which was significantly higher than that of the lead compounds and positive-control drugs Fluconazole and Itraconazole. In particular, the antifungal activity of compound 6/18 against Candida albicans and Candida krusei （MIC80 both at 0.00097 p.g/mL） was 515 and 64 times that of Fluconazole, respectively. The structure-activity relationships of the synthesized compounds were discussed, and the docking model of the target compounds with fungal lanosterol 14a-demethylase （CYP51） was analyzed.