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Focused library of phenyl-fused macrocyclic amidinoureas as antifungal agents

Lorenzo J I Balestri1, Ilaria D'Agostino1, Enrico Rango1

  • 1Department of Biotechnology, Chemistry and Pharmacy, University of Siena, 53100, Siena, Italy.

Molecular Diversity
|February 10, 2022
PubMed

Insights

New macrocyclic amidinoureas show promise against Candida and Cryptococcus fungal infections. These compounds exhibit low passive diffusion and are non-toxic, offering potential new antifungal therapies.

Area of Science:

  • Medicinal Chemistry
  • Antimicrobial Resistance
  • Mycology

Background:

  • Invasive fungal infections, particularly candidiasis, pose a significant threat to hospitalized patients, exacerbated by rising antimicrobial resistance and global pandemics.
  • The limited availability of effective antifungal drugs necessitates the development of novel therapeutic agents.

Purpose of the Study:

  • To design, synthesize, and evaluate a focused library of novel macrocyclic amidinourea derivatives with fused phenyl rings.
  • To assess the antifungal activity and preliminary mechanism of action of these new compounds against key fungal pathogens.

Main Methods:

  • Synthesis of seven macrocyclic amidinourea derivatives.
  • Antifungal activity screening against a panel of Candida species and Cryptococcus neoformans.
  • Parallel Artificial Membrane Permeability Assay (PAMPA) to investigate passive diffusion.
  • MTT assays to determine cytotoxicity.

Main Results:

  • Several synthesized compounds demonstrated significant antifungal activity against a broad spectrum of Candida spp. and C. neoformans.
  • PAMPA experiments indicated low passive diffusion for representative compounds, suggesting potential membrane-associated mechanisms or active transport involvement.
  • MTT assays confirmed that the compounds were not toxic at high concentrations.

Conclusions:

  • The novel macrocyclic amidinoureas represent a promising new class of antifungal agents with broad-spectrum activity.
  • Their low passive diffusion and lack of toxicity suggest a favorable profile for further development as potential treatments for invasive fungal infections.
Keywords:
AmidinoureaAntifungal agentsCandidaCryptococcusMacrocyclesPAMPA

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