Development of a novel family of antifungal agents based on a quinone methide oxime framework

Given the widespread occurrence of fungal infections, the phenomenon of fungal drug resistance, and the limited number of systemic antimycotic therapies, novel chemicals should be developed to control pathogenic fungi. We propose using quinone methide oximes as a novel framework for developing a novel class of antifungal agents. Compound 2 was destroyed mature biofilms at the concentration of 0.5 µg/mL (MIC/4) and prevented hyphal growth of Candida albicans at 0.125 µg/mL (MIC/16). The chemical applied at the concentration of 16-128 µg/mL inhibited the growth of the majority of the clinical isolates of Candida used, including those exhibiting resistance towards systemic drugs. Our safety studies performed with the use of normal human cells revealed that compound 2 was not toxic at the antifungal concentrations tested. Surprisingly, compound 2 showed low inhibitory activity against a set of protein kinases in comparison with its parental compound 1.

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Publication Details

Journal
Scientific Reports
Published
2025-04-18
DOI
https://doi.org/10.1038/s41598-025-98609-5
Citations
2
Primary Topic
Synthesis of Indole Derivatives
Type
article
Field-Weighted Citation Impact
1.87
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article

Development of a novel family of antifungal agents based on a quinone methide oxime framework

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2 citations
Scientific Reports
Synthesis of Indole Derivatives
1.87
article

Development of a novel family of antifungal agents based on a quinone methide oxime framework

Barbara Mirosław, Radomir Jasiński, Konrad Kubiński, Kamila Górka, Przemysław Woliński, Mateusz Kwaśnik, Béatrice Foll-Josselin, Sandrine Ruchaud, S. Bach, Maciej Masłyk, Oleg M. Demchuk, Monika Janeczko, Aleksandra Martyna, Małgorzata Sadczuk, Antonina Kurowska-Okoń
article en
2 citations

Abstract

Given the widespread occurrence of fungal infections, the phenomenon of fungal drug resistance, and the limited number of systemic antimycotic therapies, novel chemicals should be developed to control pathogenic fungi. We propose using quinone methide oximes as a novel framework for developing a novel class of antifungal agents. Compound 2 was destroyed mature biofilms at the concentration of 0.5 µg/mL (MIC/4) and prevented hyphal growth of Candida albicans at 0.125 µg/mL (MIC/16). The chemical applied at the concentration of 16-128 µg/mL inhibited the growth of the majority of the clinical isolates of Candida used, including those exhibiting resistance towards systemic drugs. Our safety studies performed with the use of normal human cells revealed that compound 2 was not toxic at the antifungal concentrations tested. Surprisingly, compound 2 showed low inhibitory activity against a set of protein kinases in comparison with its parental compound 1.

Scientific ReportsVol. 15(1)
John Paul II Catholic University of Lublin (PL), Medical University of Lublin (PL), Centre National de la Recherche Scientifique (FR), Maria Curie-Skłodowska University (PL), Station Biologique de Roscoff (FR), Sorbonne Université (FR), Cracow University of Technology (PL)
Zero hunger
Openalex Percentile: Top 16%
Synthesis of Indole Derivatives
1.87
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