Recent patents in antifungal agent discovery

Abstract

Background: Fungi are the most insidious pathogens, since they are eukaryotic microorganisms. Systemic infections are potentially fatal and are a growing danger for human health. There is increasing emergence of fungal resistance to currently available antifungal agents. Objective: An overview of the most relevant practical improvements in the field of antifungal drugs is given. Methods: A selection of the more interesting patents recorded from 2000 to 2007 is presented. Results/conclusion: Relevant news regarding azoles are the improvement of the solubility of known agents, and increased activity against Aspergillus species. Novel peptides, including echinocandins, are under study. Sordarins were analysed because they show a mechanism of action that confers on this class a high degree of selectivity. Natural products, macrolide derivatives and miscellaneous antifungals with interesting activities were described. Novel synthetic derivatives were reported as anti-Aspergillus agents. Finally, a description of compounds active on less explored targets is reported.

Keywords::

• 14α-lanosterol demethylase
• β-(1,3)-D-glucan synthase
• antifungal agent
• azole
• CYP51
• echinocandin
• efflux pump
• geranylgeranyl transferase
• macrolide
• natural product
• peptide
• polyene macrolide
• protein mannosyl transferase
• pmt
• sordarin
• translation elongation factor 2

Acknowledgements

The author thanks R Costi for her advice.