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Cyclic N, O-acetals and corresponding opened N, N-aminals as new scaffolds with promising anti-inflammatory and antifungal activities against Candida albicans
by
Daïch, Adam
, Ghinet, Alina
, Safi, Christine
, Othman, Mohamed
, Lawson, Ata Martin
, Jawhara, Samir
, Buisine, Mathys
, Camaioni, Louis
, Lambert, Dylan
in
631/92/2783
/ 631/92/60
/ 692/699/1503/257/1389
/ 692/699/1503/257/1402
/ Acetals - chemical synthesis
/ Acetals - chemistry
/ Acetals - pharmacology
/ Animals
/ Anti-inflammatory agent
/ Anti-inflammatory agents
/ Anti-Inflammatory Agents - chemical synthesis
/ Anti-Inflammatory Agents - chemistry
/ Anti-Inflammatory Agents - pharmacology
/ Antifungal activity
/ Antifungal agents
/ Antifungal Agents - chemical synthesis
/ Antifungal Agents - chemistry
/ Antifungal Agents - pharmacology
/ Biofilms
/ Biofilms - drug effects
/ Caenorhabditis elegans - drug effects
/ Caenorhabditis elegans - microbiology
/ Candida albicans
/ Candida albicans - drug effects
/ Candidiasis - drug therapy
/ Caspofungin
/ Chemical Sciences
/ Clinical isolates
/ Fluconazole
/ Gene expression
/ Humanities and Social Sciences
/ Humans
/ Inflammation
/ Inflammatory diseases
/ Interleukin-1beta - metabolism
/ Macrophages
/ Macrophages - drug effects
/ Macrophages - metabolism
/ Mice
/ Microbial Sensitivity Tests
/ multidisciplinary
/ N,N-aminals
/ N,O-acetals
/ NF-kappa B - metabolism
/ NF-κB protein
/ Pathogenesis
/ RAW 264.7 Cells
/ Reactive Oxygen Species - metabolism
/ Science
/ Science (multidisciplinary)
2025
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Cyclic N, O-acetals and corresponding opened N, N-aminals as new scaffolds with promising anti-inflammatory and antifungal activities against Candida albicans
by
Daïch, Adam
, Ghinet, Alina
, Safi, Christine
, Othman, Mohamed
, Lawson, Ata Martin
, Jawhara, Samir
, Buisine, Mathys
, Camaioni, Louis
, Lambert, Dylan
in
631/92/2783
/ 631/92/60
/ 692/699/1503/257/1389
/ 692/699/1503/257/1402
/ Acetals - chemical synthesis
/ Acetals - chemistry
/ Acetals - pharmacology
/ Animals
/ Anti-inflammatory agent
/ Anti-inflammatory agents
/ Anti-Inflammatory Agents - chemical synthesis
/ Anti-Inflammatory Agents - chemistry
/ Anti-Inflammatory Agents - pharmacology
/ Antifungal activity
/ Antifungal agents
/ Antifungal Agents - chemical synthesis
/ Antifungal Agents - chemistry
/ Antifungal Agents - pharmacology
/ Biofilms
/ Biofilms - drug effects
/ Caenorhabditis elegans - drug effects
/ Caenorhabditis elegans - microbiology
/ Candida albicans
/ Candida albicans - drug effects
/ Candidiasis - drug therapy
/ Caspofungin
/ Chemical Sciences
/ Clinical isolates
/ Fluconazole
/ Gene expression
/ Humanities and Social Sciences
/ Humans
/ Inflammation
/ Inflammatory diseases
/ Interleukin-1beta - metabolism
/ Macrophages
/ Macrophages - drug effects
/ Macrophages - metabolism
/ Mice
/ Microbial Sensitivity Tests
/ multidisciplinary
/ N,N-aminals
/ N,O-acetals
/ NF-kappa B - metabolism
/ NF-κB protein
/ Pathogenesis
/ RAW 264.7 Cells
/ Reactive Oxygen Species - metabolism
/ Science
/ Science (multidisciplinary)
2025
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Cyclic N, O-acetals and corresponding opened N, N-aminals as new scaffolds with promising anti-inflammatory and antifungal activities against Candida albicans
by
Daïch, Adam
, Ghinet, Alina
, Safi, Christine
, Othman, Mohamed
, Lawson, Ata Martin
, Jawhara, Samir
, Buisine, Mathys
, Camaioni, Louis
, Lambert, Dylan
in
631/92/2783
/ 631/92/60
/ 692/699/1503/257/1389
/ 692/699/1503/257/1402
/ Acetals - chemical synthesis
/ Acetals - chemistry
/ Acetals - pharmacology
/ Animals
/ Anti-inflammatory agent
/ Anti-inflammatory agents
/ Anti-Inflammatory Agents - chemical synthesis
/ Anti-Inflammatory Agents - chemistry
/ Anti-Inflammatory Agents - pharmacology
/ Antifungal activity
/ Antifungal agents
/ Antifungal Agents - chemical synthesis
/ Antifungal Agents - chemistry
/ Antifungal Agents - pharmacology
/ Biofilms
/ Biofilms - drug effects
/ Caenorhabditis elegans - drug effects
/ Caenorhabditis elegans - microbiology
/ Candida albicans
/ Candida albicans - drug effects
/ Candidiasis - drug therapy
/ Caspofungin
/ Chemical Sciences
/ Clinical isolates
/ Fluconazole
/ Gene expression
/ Humanities and Social Sciences
/ Humans
/ Inflammation
/ Inflammatory diseases
/ Interleukin-1beta - metabolism
/ Macrophages
/ Macrophages - drug effects
/ Macrophages - metabolism
/ Mice
/ Microbial Sensitivity Tests
/ multidisciplinary
/ N,N-aminals
/ N,O-acetals
/ NF-kappa B - metabolism
/ NF-κB protein
/ Pathogenesis
/ RAW 264.7 Cells
/ Reactive Oxygen Species - metabolism
/ Science
/ Science (multidisciplinary)
2025
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Cyclic N, O-acetals and corresponding opened N, N-aminals as new scaffolds with promising anti-inflammatory and antifungal activities against Candida albicans
Journal Article
Cyclic N, O-acetals and corresponding opened N, N-aminals as new scaffolds with promising anti-inflammatory and antifungal activities against Candida albicans
2025
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Overview
P2 × 7R is crucial in the pathogenesis of chronic inflammatory diseases, and its activation leads to the release of pro-inflammatory cytokines, exacerbating the inflammatory response. Two new series of scarce cyclic
N
,
O
-acetals (ATF 61–74) and corresponding opened
N
,
N
-aminals (CS 1–14) have been designed as novel potential P2RX7 antagonists, then synthesized and evaluated for their anti-inflammatory properties through investigating the pro-inflammatory markers and also for their antifungal activity against
Candida albicans
. Three compounds (ATF 64, CS 8, and CS 9) exhibited dual antifungal and anti-inflammatory properties. ATF 64, CS 8, and CS 9 reduced ROS production and IL-1β expression in macrophages and intestinal cells in a manner correlated with NF-KB expression. These compounds showed excellent antifungal activity against clinical isolates of
C. albicans
resistant to fluconazole and caspofungin, and reduced
C. albicans
biofilm formation. Treatment with CS 8 or CS 9 protected the nematode
Caenorhabditis elegans
against infection with
C. albicans
and enhanced antimicrobial gene expression. This duality of action offers a promising new pharmacological strategy to counteract inflammatory diseases and propels
N
,
N
-aminals as promising candidates for future optimization and investigation.
Publisher
Nature Publishing Group UK,Nature Publishing Group,Nature Portfolio
Subject
/ Acetals - chemical synthesis
/ Animals
/ Anti-Inflammatory Agents - chemical synthesis
/ Anti-Inflammatory Agents - chemistry
/ Anti-Inflammatory Agents - pharmacology
/ Antifungal Agents - chemical synthesis
/ Antifungal Agents - chemistry
/ Antifungal Agents - pharmacology
/ Biofilms
/ Caenorhabditis elegans - drug effects
/ Caenorhabditis elegans - microbiology
/ Candida albicans - drug effects
/ Humanities and Social Sciences
/ Humans
/ Interleukin-1beta - metabolism
/ Mice
/ Reactive Oxygen Species - metabolism
/ Science
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