Design and synthesis of novel triazole derivatives containing γ-lactam as potential antifungal agents

作     者：Yuan-Yuan Xu An-Ran Qian Xu-Feng Cao Chen-Yu Ling Yong-Bing Cao Rui-Lian Wang Yi-Su Li Yu-She Yang 

作者机构：State Key Laboratory of Drug Research Shanghai Institute of Materia Medica Shanghai Institute for Biological Sciences Chinese Academy of Sciences Shanghai 201203 China School of Pharmacy Second Military Medical University Shanghai 200433 China Drug Discovery and Design Center State Key Laboratory of Drug Research Shanghai Institute of Materia Medica Chinese Academy of Sciences Shanghai 201203 China 

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

年 卷 期：2016年第27卷第5期

页      面：703-706页

核心收录：

学科分类：08[工学] 080501[工学-材料物理与化学] 0805[工学-材料科学与工程（可授工学、理学学位）] 0703[理学-化学] 

基　　金：supported by the National Natural Science Foundation of China (No. 21402223) 

主　　题：Synthesis Triazole γ Lactam Antifungal activity 

摘      要：A series of novel triazole derivatives containing y-lactam were designed and synthesized, and their structures were confirmed by IH NMR, 13C NMR and HRMS, The in vitro antifungal activities of the target compounds were evaluated, The results showed that all of the compounds exhibited stronger activity against the six clinically important fungi tested than fluconazole. 3D and 3E showed comparative activity against the fungi tested except for Candida glabrata and Aspergillus fumigatus as voriconazole. In addition, the docking model for 2A and CYP51 was investigated.