Two New Compounds Containing Pyridinone or Triazine Heterocycles Have Antifungal Properties against <i>Candida albicans</i>
Candidiasis, caused by the opportunistic yeast <i>Candida albicans</i>, is the most common fungal infection today. Resistance of <i>C. albicans</i> to current antifungal drugs has emerged over the past decade leading to the need for novel antifungal agents. Our aim was to sel...
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| Main Authors: | , , , , , , |
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| Format: | Book |
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MDPI AG,
2022-01-01T00:00:00Z.
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| Summary: | Candidiasis, caused by the opportunistic yeast <i>Candida albicans</i>, is the most common fungal infection today. Resistance of <i>C. albicans</i> to current antifungal drugs has emerged over the past decade leading to the need for novel antifungal agents. Our aim was to select new antifungal compounds by library-screening methods and to assess their antifungal effects against <i>C. albicans</i>. After screening 90 potential antifungal compounds from JUNIA, a chemical library, two compounds, 1-(4-chlorophenyl)-4-((4-chlorophenyl)amino)-3,6-dimethylpyridin-2(1<i>H</i>)-one (PYR) and (<i>Z</i>)-<i>N</i>-(2-(4,6-dimethoxy-1,3,5-triazin-2-yl)vinyl)-4-methoxyaniline (TRI), were identified as having potential antifungal activity. Treatment with PYR and TRI resulted in a significant reduction of <i>C. albicans</i> bioluminescence as well as the number of fungal colonies, indicating rapid fungicidal activity. These two compounds were also effective against clinically isolated fluconazole- or caspofungin-resistant <i>C. albicans</i> strains. PYR and TRI had an inhibitory effect on <i>Candida</i> biofilm formation and reduced the thickness of the mannan cell wall. In a <i>Caenorhabditis elegans</i> infection model, PYR and TRI decreased the mortality of nematodes infected with <i>C. albicans</i> and enhanced the expression of antimicrobial genes that promote <i>C. albicans</i> elimination. Overall, PYR and TRI showed antifungal properties against <i>C. albicans</i> by exerting fungicidal activities and enhancing the antimicrobial gene expression of <i>Caenorhabditis elegans</i>. |
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| Item Description: | 10.3390/antibiotics11010072 2079-6382 |