Novel antifungal agents: a patent review (2011 – present)

Abstract

Introduction: Invasive fungal infections (IFI) have increased significantly over the past decades. The mortality rate of IFI is alarming, and early and accurate diagnosis is difficult. Most used antifungal drugs are not completely effective due to the development of increasing resistance and undesirable side effects which limit their use. In this scenario, new effective broad spectrum and safer antifungal drugs are urgently needed.

Areas covered: This review summarizes the latest advances in the discovery of new antifungal compounds through the patents granted from 2011 to August 2013. In the 26 patents reviewed here, either derivatives of existing antifungal drugs or novel structures are included. New imidazoles, fluconazole analogs and adducts of azoles with 2,6-di-tert-butyl-4-methylphenol are described. The review also includes chitinases, β-1,3-D-glucan and chitin synthases inhibitors and novel structures.

Expert opinion: In the patents reviewed here, progress has been made to accomplish at least one of the necessary requirements for the development of novel antifungal agents, such as broad spectrum of activity, more favorable pharmacokinetic profile, good bioavailability and low adverse effects. However, in vivo activity, mechanisms of action, drug–drug interactions and other aspects that make a compound a good antifungal agent need further development.

Keywords::

• antifungal compounds
• azole
• drug resistance
• echinocandins
• ergosterol biosynthesis inhibition
• fungal cell wall
• fungal membrane

Acknowledgments

G Crespo from Fundación Medina (Granada, España) provided assistance for MCM and FV with the ChemDraw software. The review was conducted by both authors F Vicente and SA Zacchino.

Notes

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