Antifungal activity of substituted aurones

doi:10.1016/j.bmcl.2017.01.012

Bioorganic & Medicinal Chemistry Letters

Volume 27, Issue 4, 15 February 2017, Pages 901-903

https://doi.org/10.1016/j.bmcl.2017.01.012 Get rights and content

Abstract

Novel antifungals are in high demand as there is a growing resistance to antifungals currently in use. In particular, opportunistic fungal infections caused by Candida spp. are on the rise with infections by this genus accounting for the most severe fungal infections following chemotherapy, implantation procedures, and in patients with HIV/AIDS. A series of simple aurone analogs were synthesized and screened for antifungal activity versus Candida spp. Several compounds displayed activity at 100 μM, with two having IC₅₀ values below 20 μM for three species of Candida. One of the compounds tested here also exhibits anti-biofilm activity for mid-maturation growth.

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Acknowledgements

The authors acknowledge support from Middle Tennessee State University and the Tennessee Center for Botanical Medicinal Research.

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Aurones are naturally occurring structural isomerides of flavones that have diverse bioactivities including antiviral, antibacterial, antifungal, anti-inflammatory, antitumor, antimalarial, antioxidant, neuropharmacological activities and so on. They constitute an important class of pharmacologically active scaffolds that exhibit multiple biological activities via diverse mechanisms. This review article provides an update on the recent advances (2013–2020.4) in the synthesis and biological activities of these derivatives. In the cases where sufficient information is available, some important structure–activity relationships (SAR) of their biological activities were presented, and on the strength of our expertise in medicinal chemistry and careful analysis of the recent literature, for the potential of aurones as medicinal drugs is proposed.
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Antifungal activity of substituted aurones

Abstract

Graphical abstract

Section snippets

Acknowledgements

Virulence

Antimicrob Agents Chemother

Clin Microbiol Rev

Antimicrob Agents Chemother

Antimicrob Agents Chemother

Drug Intell Clin Pharm

Antimicrob Agents Chemother

Clin Microbiol Rev

Clin Microbiol Rev

Am J Med