Benzimidazole tethered pyrrolo[3,4-b]quinoline with broad-spectrum activity against fungal pathogens

• Published in: Bioorganic & medicinal chemistry letters Vol. 29; no. 5; pp. 729 - 733
• Main Authors: Villa, Pedro, Arumugam, Natarajan, Almansour, Abdulrahman I., Suresh Kumar, Raju, Mahalingam, S.M., Maruoka, Keiji, Thangamani, Shankar
• Format: Journal Article
• Language: English
• Published: England Elsevier Ltd 01.03.2019
• Subjects: Antifungal agent; Antifungal Agents - pharmacology; Benzimidazole fused pyrroloquinoline; Benzimidazoles - chemistry; Biofilms - drug effects; Candida albicans - drug effects; Cryptococcus - drug effects; Microbial Sensitivity Tests; Povarov reaction; Pyrroles - chemistry; Quinolines - chemistry; Toxicity; Antifungal agent; Povarov reaction; Benzimidazole fused pyrroloquinoline; Toxicity
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/j.bmcl.2019.01.006

Antifungal activities of benzimidazole tethered pyrrolo[3,4-b]quinoline compounds. [Display omitted] Fungal infections caused by Candida and Cryptococcus are particularly dangerous for immunocompromised individuals. In this study, we identified that benzimidazole fused pyrrolo[3,4-b]quinoline compounds have potent antifungal activity against several clinical isolates of pathogenic fungal strains. Specifically, the compound 6a did not show cytotoxicity against mammalian cells at a concentration that inhibits the growth of fungal strains. In addition, the compound 6a also significantly reduced the metabolic activity of fungal cells in the Candida albicans biofilms. Collectively, our results indicate that benzimidazole fused quinoline compounds have a potential to develop as an antifungal agents.