Extended Antimicrobial Profile of Chromone–Butenafine Hybrids

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 <b>3</b> a promising activity towards <i>C. auris</i>, <i>C. tropicalis</i>, and <i>C. neoformans</i>, for which a high degree of resistance is commonly observed, together with a significant antibacterial potency towards Gram-positive bacteria, such as <i>S. aureus</i>. Considering that compound <b>3</b> displayed favorable selectivity and therapeutic indexes (9.1 and >16, respectively), it appeared as a valuable prototype, deserving further hit-to-lead optimization.

Abstract licence: CC BY

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