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Title: | Focused library of phenyl-fused macrocyclic amidinoureas as antifungal agents | Authors: | Balestri, Lorenzo J I D'Agostino, Ilaria Rango, Enrico Vagaggini, Chiara Marchitiello, Rosalba Mariotti, Melinda Casian, Alexandru Deodato, Davide Truglio, Giuseppina I Orofino, Francesco Sanguinetti, Maurizio Bugli, Francesca Lorenzo Botta Dreassi, Elena |
Journal: | MOLECULAR DIVERSITY | Issue Date: | 2022 | Abstract: | The rise of antimicrobial-resistant phenotypes and the spread of the global pandemic of COVID-19 are worsening the outcomes of hospitalized patients for invasive fungal infections. Among them, candidiases are seriously worrying, especially since the currently available drug armamentarium is extremely limited. We recently reported a new class of macrocyclic amidinoureas bearing a guanidino tail as promising antifungal agents. Herein, we present the design and synthesis of a focused library of seven derivatives of macrocyclic amidinoureas, bearing a second phenyl ring fused with the core. Biological activity evaluation shows an interesting antifungal profile for some compounds, resulting to be active on a large panel of Candida spp. and C. neoformans. PAMPA experiments for representative compounds of the series revealed a low passive diffusion, suggesting a membrane-based mechanism of action or the involvement of active transport systems. Also, compounds were found not toxic at high concentrations, as assessed through MTT assays. |
URI: | http://hdl.handle.net/2067/47200 | ISSN: | 1381-1991 | DOI: | 10.1007/s11030-022-10388-7 | Rights: | Attribution-NonCommercial-ShareAlike 4.0 International |
Appears in Collections: | A1. Articolo in rivista |
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Balestri2022_Article_FocusedLibraryOfPhenyl-fusedMa.pdf | Article | 1.7 MB | Adobe PDF | Request a copy |
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