Two New Compounds Containing Pyridinone ...
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Article dans une revue scientifique: Article original
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Title :
Two New Compounds Containing Pyridinone or Triazine Heterocycles Have Antifungal Properties against Candida albicans
Author(s) :
Mena, Laura [Auteur]
Unité de Glycobiologie Structurale et Fonctionnelle - UMR 8576 [UGSF]
Service de Parasitologie-Mycologie [CHRU LIlle]
Faculté de Médecine Henri Warembourg - Université de Lille
Billamboz, Muriel [Auteur]
Facteurs de risque et déterminants moléculaires des maladies liées au vieillissement (RID-AGE) - U1167
JUNIA [JUNIA]
Charlet, Rogatien [Auteur]
Unité de Glycobiologie Structurale et Fonctionnelle (UGSF) - UMR 8576
Service de Parasitologie-Mycologie [CHRU LIlle]
Faculté de Médecine Henri Warembourg - Université de Lille
Desprès, Bérangère [Auteur]
Unité de Glycobiologie Structurale et Fonctionnelle - UMR 8576 [UGSF]
Service de Parasitologie-Mycologie [CHRU LIlle]
Faculté de Médecine Henri Warembourg - Université de Lille
Sendid, Boualem [Auteur]
Unité de Glycobiologie Structurale et Fonctionnelle (UGSF) - UMR 8576
Service de Parasitologie-Mycologie [CHRU LIlle]
Faculté de Médecine Henri Warembourg - Université de Lille
Ghinet, Alina [Auteur]
Facteurs de risque et déterminants moléculaires des maladies liées au vieillissement (RID-AGE) - U1167
JUNIA [JUNIA]
Alexandru Ioan Cuza University of Iași [Romania]
Jawhara, Samir [Auteur]
Unité de Glycobiologie Structurale et Fonctionnelle (UGSF) - UMR 8576
Service de Parasitologie-Mycologie [CHRU LIlle]
Faculté de Médecine Henri Warembourg - Université de Lille
Unité de Glycobiologie Structurale et Fonctionnelle - UMR 8576 [UGSF]
Service de Parasitologie-Mycologie [CHRU LIlle]
Faculté de Médecine Henri Warembourg - Université de Lille
Billamboz, Muriel [Auteur]

Facteurs de risque et déterminants moléculaires des maladies liées au vieillissement (RID-AGE) - U1167
JUNIA [JUNIA]
Charlet, Rogatien [Auteur]
Unité de Glycobiologie Structurale et Fonctionnelle (UGSF) - UMR 8576
Service de Parasitologie-Mycologie [CHRU LIlle]
Faculté de Médecine Henri Warembourg - Université de Lille
Desprès, Bérangère [Auteur]
Unité de Glycobiologie Structurale et Fonctionnelle - UMR 8576 [UGSF]
Service de Parasitologie-Mycologie [CHRU LIlle]
Faculté de Médecine Henri Warembourg - Université de Lille
Sendid, Boualem [Auteur]
Unité de Glycobiologie Structurale et Fonctionnelle (UGSF) - UMR 8576
Service de Parasitologie-Mycologie [CHRU LIlle]
Faculté de Médecine Henri Warembourg - Université de Lille
Ghinet, Alina [Auteur]

Facteurs de risque et déterminants moléculaires des maladies liées au vieillissement (RID-AGE) - U1167
JUNIA [JUNIA]
Alexandru Ioan Cuza University of Iași [Romania]
Jawhara, Samir [Auteur]
Unité de Glycobiologie Structurale et Fonctionnelle (UGSF) - UMR 8576
Service de Parasitologie-Mycologie [CHRU LIlle]
Faculté de Médecine Henri Warembourg - Université de Lille
Journal title :
Antibiotics
Abbreviated title :
Antibiotics
Volume number :
11
Pages :
72
Publisher :
MDPI AG
Publication date :
2022-01-08
ISSN :
2079-6382
English keyword(s) :
Candida albicans
antifungal agents
biofilm formation
C. elegans infection model
antifungal agents
biofilm formation
C. elegans infection model
HAL domain(s) :
Sciences du Vivant [q-bio]
Chimie/Chimie théorique et/ou physique
Chimie/Chimie théorique et/ou physique
English abstract : [en]
Candidiasis, caused by the opportunistic yeast Candida albicans, is the most common fungal infection today. Resistance of C. albicans to current antifungal drugs has emerged over the past decade leading to the need for ...
Show more >Candidiasis, caused by the opportunistic yeast Candida albicans, is the most common fungal infection today. Resistance of C. albicans 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 C. albicans. After screening 90 potential antifungal compounds from JUNIA, a chemical library, two compounds, 1-(4-chlorophenyl)-4-((4-chlorophenyl)amino)-3,6-dimethylpyridin-2(1H)-one (PYR) and (Z)-N-(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 C. albicans 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 C. albicans strains. PYR and TRI had an inhibitory effect on Candida biofilm formation and reduced the thickness of the mannan cell wall. In a Caenorhabditis elegans infection model, PYR and TRI decreased the mortality of nematodes infected with C. albicans and enhanced the expression of antimicrobial genes that promote C. albicans elimination. Overall, PYR and TRI showed antifungal properties against C. albicans by exerting fungicidal activities and enhancing the antimicrobial gene expression of Caenorhabditis elegans.Show less >
Show more >Candidiasis, caused by the opportunistic yeast Candida albicans, is the most common fungal infection today. Resistance of C. albicans 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 C. albicans. After screening 90 potential antifungal compounds from JUNIA, a chemical library, two compounds, 1-(4-chlorophenyl)-4-((4-chlorophenyl)amino)-3,6-dimethylpyridin-2(1H)-one (PYR) and (Z)-N-(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 C. albicans 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 C. albicans strains. PYR and TRI had an inhibitory effect on Candida biofilm formation and reduced the thickness of the mannan cell wall. In a Caenorhabditis elegans infection model, PYR and TRI decreased the mortality of nematodes infected with C. albicans and enhanced the expression of antimicrobial genes that promote C. albicans elimination. Overall, PYR and TRI showed antifungal properties against C. albicans by exerting fungicidal activities and enhancing the antimicrobial gene expression of Caenorhabditis elegans.Show less >
Language :
Anglais
Audience :
Internationale
Popular science :
Non
Administrative institution(s) :
Université de Lille
CNRS
CNRS
Collections :
Research team(s) :
Glycobiology in fungal Pathogenesis and Clinical Applications
Submission date :
2023-01-18T09:21:17Z
2023-01-18T15:35:10Z
2023-01-18T15:35:10Z
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