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Allylamine type xanthone antimycotics

I Salmoiraghi1, M Rossi, P Valenti

  • 1Institute of Pharmaceutical Chemistry, University of Milan, Italy.

Archiv Der Pharmazie
|August 26, 1998
PubMed
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New xanthone derivatives were synthesized and tested for antifungal properties. Butenafine-based xanthone analogs demonstrated significant activity against Cryptococcus neoformans, with regioisomer 4d showing particular potency.

Area of Science:

  • Medicinal Chemistry
  • Mycology
  • Organic Synthesis

Background:

  • Antifungal drug discovery is crucial for treating infections caused by molds and yeasts.
  • Naftifine and butenafine are established allylamine antifungal agents.
  • Xanthone scaffolds are explored for novel therapeutic applications.

Purpose of the Study:

  • To synthesize novel xanthone derivatives incorporating the side chains of naftifine and butenafine.
  • To evaluate the in vitro antifungal activity of these novel compounds.
  • To identify potent antifungal agents, particularly against challenging fungal pathogens.

Main Methods:

  • Synthesis of xanthone derivatives with basic side chains at nuclear positions 1, 2, 3, and 4.
  • In vitro antifungal screening against various mold and yeast strains.

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  • Determination of minimum inhibitory concentrations (MICs) for active compounds.
  • Main Results:

    • Several xanthone derivatives were successfully synthesized.
    • Butenafine-based xanthone analogs exhibited significant antifungal activity.
    • Regioisomer 4d, a butenafine xanthone analog, showed potent activity against Cryptococcus neoformans with an MIC of 1.5 µg/ml.

    Conclusions:

    • Butenafine xanthone analogs represent a promising class of antifungal compounds.
    • Regioisomer 4d is a highly effective inhibitor of Cryptococcus neoformans growth.
    • Further investigation into these derivatives may lead to new antifungal therapies.