Design, synthesis and antifungal activity of carbazole derivatives

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.

Graphical abstractThe structure–activity relationship of a tetrahydrocarbazole antifungal lead compound was investigated. Several targeted compounds showed potent activity against Candida species. Particularly, the most active compound 13i can be used as a good starting point for the discovery of novel antifungal agents.Figure optionsDownload full-size imageDownload as PowerPoint slide