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
• 机 构: School of Pharmacy,Second Military Medical University,
• 出 处: Chinese Chemical Letters
• 发表日期: 2014年02期
• 关键词: antifungal carbazole scaffold urgent Candida fungal potent targeted chains start

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.

The incidence of invasive fungal infections is increasing rapidly. Clinically available antifungal agents suffer from limited efficacy and severe resistance. Here 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 .