Design,synthesis and antifungal activity of carbazole derivatives

作     者：Shi-Ping Zhu Wen-Ya Wang Kun Fang Zheng-Gang Li Guo-Qiang Dong Zhen-Yuan Miao Jian-Zhong Yao Wan-Nian Zhang Chun-Quan Sheng 

作者机构：School of PharmacySecond Military Medical University 

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

年 卷 期：2014年第25卷第2期

页      面：229-233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 in part by the National Natural Science Foundation of China(No.81222044) the 863 Hi-Tech Program of China(No.2012AA020302) Shanghai Rising-Star Program(No.12QH1402600) Shanghai Municipal Health Bureau(No.XYQ2011038) 

主　　题：Carbazol Antifungal activity Structure-activity relationship 

摘      要：The incidence of invasive fungal infections is increasing rapidly. Clinically available antifungal agents suffer from limited efficacy and severe resistance. There is an urgent need to discover antifungal lead compounds with novel chemical scaffold. On the basis of our previously identified tetrahydrocarbazole antifungal leads, the structure-activity relationship was further explored by modifying the scaffold and the side chains. Several targeted compounds showed potent activity against Candida species. Particularly, compound 13i showed better antifungal activity than the lead compound, which can be used as a good starting point for further optimization.