Fungal infections are recognized as a global health issue, in particular considering the spread of different forms of resistance to the commonly used antifungal drugs and their involvement in the occurrence of co-infections in hospitalized and immunocompromised patients. In this paper, a small series of hybrid compounds were designed and synthesized by linking the privileged chromone and xanthone scaffolds, endowed with recognized antimicrobial potential, to the tert-butylbenzylamino portion of the antifungal drug butenafine, through selected linkers. The results showed for the xanthone-based compound 3 a promising activity towards C. auris, C. tropicalis, and C. neoformans, for which a high degree of resistance is commonly observed, together with a significant antibacterial potency towards Gram-positive bacteria, such as S. aureus. Considering that compound 3 displayed favorable selectivity and therapeutic indexes (9.1 and >16, respectively), it appeared as a valuable prototype, deserving further hit-to-lead optimization.
Bonvicini, F., Menegaldo, L., Orioli, R., Belluti, F., Gentilomi, G.A., Gobbi, S., et al. (2025). Extended Antimicrobial Profile of Chromone–Butenafine Hybrids. MOLECULES, 30(14), 1-16 [10.3390/molecules30142973].
Extended Antimicrobial Profile of Chromone–Butenafine Hybrids
Bonvicini F.
;Menegaldo L.;Orioli R.;Belluti F.;Gentilomi G. A.;Gobbi S.;Bisi A.
2025
Abstract
Fungal infections are recognized as a global health issue, in particular considering the spread of different forms of resistance to the commonly used antifungal drugs and their involvement in the occurrence of co-infections in hospitalized and immunocompromised patients. In this paper, a small series of hybrid compounds were designed and synthesized by linking the privileged chromone and xanthone scaffolds, endowed with recognized antimicrobial potential, to the tert-butylbenzylamino portion of the antifungal drug butenafine, through selected linkers. The results showed for the xanthone-based compound 3 a promising activity towards C. auris, C. tropicalis, and C. neoformans, for which a high degree of resistance is commonly observed, together with a significant antibacterial potency towards Gram-positive bacteria, such as S. aureus. Considering that compound 3 displayed favorable selectivity and therapeutic indexes (9.1 and >16, respectively), it appeared as a valuable prototype, deserving further hit-to-lead optimization.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
