Synthesis of new linear guanidines and macrocyclic amidinourea derivatives endowed with high antifungal activity against Candida spp. and Aspergillus spp.

Fabrizio Manetti, Daniele Castagnolo, Francesco Raffi, Alessandra T. Zizzari, Suvi Rajamaki, Silvia D'Arezzo, Paolo Visca, Alessandra Cona, Maria Enrica Fracasso, Denise Doria, Brunella Posteraro, Maurizio Sanguinetti, Giovanni Fadda, Maurizio Botta

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Abstract

New linear and cyclic guanidines were synthesized and tested in vitro for their antifungal activity toward clinically relevant strains of Candida species, in comparison to fluconazole. Macrocyclic compounds showed a minimum inhibitory concentration in the micromolar range and a biological activity profile in some cases better than that of fluconazole. One macrocyclic derivative was also tested against Aspergillus species and showed high antifungal activity comparable to that of amphotericin B and itraconazole.

Original languageEnglish
Pages (from-to)7376-7379
Number of pages4
JournalJournal of Medicinal Chemistry
Volume52
Issue number23
DOIs
Publication statusPublished - Dec 10 2009

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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  • Cite this

    Manetti, F., Castagnolo, D., Raffi, F., Zizzari, A. T., Rajamaki, S., D'Arezzo, S., Visca, P., Cona, A., Fracasso, M. E., Doria, D., Posteraro, B., Sanguinetti, M., Fadda, G., & Botta, M. (2009). Synthesis of new linear guanidines and macrocyclic amidinourea derivatives endowed with high antifungal activity against Candida spp. and Aspergillus spp. Journal of Medicinal Chemistry, 52(23), 7376-7379. https://doi.org/10.1021/jm900760k