Synthesis and Antifungal Activity of Perylene Bisimide Derivatives

Abstract

In this study, we have synthesized several perylene bisimide derivatives and evaluated the antifungal activity against human pathogenic yeasts (Candida spp.) and filamentous fungi (Aspergillus spp., Fusarium spp., and Trichophyton spp.). Three compounds (2-4) from the nine compounds tested presented relevant activity against Candida albicans, C. parapsilosis and C. tropicalis with minimum inhibitory concentrations (MIC 90) values of 3.1-25.0 µg/mL. These three compounds also showed activity against filamentous fungi, F. oxysporum, T. rubrum and T. mentagrophytes at a concentration of 50 µg/mL. The resultant data indicates that perylene bisimides (2-4) display wide spectrum and relevant antifungal activity. Compound 4 represents a new scaffold for the development of antifungal agents and warrant further structure activity relationship studies.