Second generation of thiazolylmannosides, ...
Document type :
Article dans une revue scientifique
DOI :
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Title :
Second generation of thiazolylmannosides, FimH antagonists for E. coli-induced Crohn's disease
Author(s) :
Chalopin, Thibaut [Auteur]
Chimie Et Interdisciplinarité : Synthèse, Analyse, Modélisation [CEISAM]
Alvarez Dorta, Dimitri [Auteur]
Chimie Et Interdisciplinarité : Synthèse, Analyse, Modélisation [CEISAM]
Sivignon, Adeline [Auteur]
Institut National de la Santé et de la Recherche Médicale [INSERM]
Institut National de la Recherche Agronomique [INRA]
Caudan, M. [Auteur]
Chimie Et Interdisciplinarité : Synthèse, Analyse, Modélisation [CEISAM]
Dumych, T. I. [Auteur]
Unité de Glycobiologie Structurale et Fonctionnelle - UMR 8576 [UGSF]
Bilyy, R. O. [Auteur]
Deniaud, David [Auteur]
Chimie Et Interdisciplinarité : Synthèse, Analyse, Modélisation [CEISAM]
Barnich, Nicolas [Auteur]
Institut National de la Santé et de la Recherche Médicale [INSERM]
Institut National de la Recherche Agronomique [INRA]
Bouckaert, Julie [Auteur]
Unité de Glycobiologie Structurale et Fonctionnelle - UMR 8576 [UGSF]
Gouin, S. G. [Auteur]
Chimie Et Interdisciplinarité : Synthèse, Analyse, Modélisation [CEISAM]
Chimie Et Interdisciplinarité : Synthèse, Analyse, Modélisation [CEISAM]
Alvarez Dorta, Dimitri [Auteur]
Chimie Et Interdisciplinarité : Synthèse, Analyse, Modélisation [CEISAM]
Sivignon, Adeline [Auteur]
Institut National de la Santé et de la Recherche Médicale [INSERM]
Institut National de la Recherche Agronomique [INRA]
Caudan, M. [Auteur]
Chimie Et Interdisciplinarité : Synthèse, Analyse, Modélisation [CEISAM]
Dumych, T. I. [Auteur]
Unité de Glycobiologie Structurale et Fonctionnelle - UMR 8576 [UGSF]
Bilyy, R. O. [Auteur]
Deniaud, David [Auteur]
Chimie Et Interdisciplinarité : Synthèse, Analyse, Modélisation [CEISAM]
Barnich, Nicolas [Auteur]
Institut National de la Santé et de la Recherche Médicale [INSERM]
Institut National de la Recherche Agronomique [INRA]
Bouckaert, Julie [Auteur]

Unité de Glycobiologie Structurale et Fonctionnelle - UMR 8576 [UGSF]
Gouin, S. G. [Auteur]
Chimie Et Interdisciplinarité : Synthèse, Analyse, Modélisation [CEISAM]
Journal title :
Organic & Biomolecular Chemistry
Abbreviated title :
Org. Biomol. Chem.
Volume number :
14
Pages :
3913-3925
Publication date :
2016-04-28
ISSN :
1477-0539
English keyword(s) :
Microbial Sensitivity Tests
Fimbriae Proteins
Mannosides
Enzyme-Linked Immunosorbent Assay
Magnetic Resonance Spectroscopy
Adhesins, Escherichia coli
Humans
Escherichia coli
Thiazoles
Crohn Disease
Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization
Fimbriae Proteins
Mannosides
Enzyme-Linked Immunosorbent Assay
Magnetic Resonance Spectroscopy
Adhesins, Escherichia coli
Humans
Escherichia coli
Thiazoles
Crohn Disease
Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization
HAL domain(s) :
Chimie/Chimie théorique et/ou physique
Sciences du Vivant [q-bio]/Microbiologie et Parasitologie/Bactériologie
Sciences du Vivant [q-bio]/Microbiologie et Parasitologie/Bactériologie
English abstract : [en]
The anti-adhesive strategy, consisting of disrupting bacterial attachment to the host cells, is widely explored as an alternative to antibiotic therapies. Recently, thiazolylmannosides (TazMans) have been identified as ...
Show more >The anti-adhesive strategy, consisting of disrupting bacterial attachment to the host cells, is widely explored as an alternative to antibiotic therapies. Recently, thiazolylmannosides (TazMans) have been identified as strong anti-adhesives of E. coli strains implied in the gut inflammation of patients with Crohn's disease. In this work, we developed a second generation of TazMans with improved chemical stability. The anomeric nitrogen was substituted by short linkers and the compounds were assessed against the bacterial adhesin FimH and the clinically isolated LF82 E. coli strain in four in vitro assays. The results obtained on the FimH adhesin alone and the whole bacteria enabled the identification of a candidate for further in vivo evaluations.Show less >
Show more >The anti-adhesive strategy, consisting of disrupting bacterial attachment to the host cells, is widely explored as an alternative to antibiotic therapies. Recently, thiazolylmannosides (TazMans) have been identified as strong anti-adhesives of E. coli strains implied in the gut inflammation of patients with Crohn's disease. In this work, we developed a second generation of TazMans with improved chemical stability. The anomeric nitrogen was substituted by short linkers and the compounds were assessed against the bacterial adhesin FimH and the clinically isolated LF82 E. coli strain in four in vitro assays. The results obtained on the FimH adhesin alone and the whole bacteria enabled the identification of a candidate for further in vivo evaluations.Show less >
Language :
Anglais
Audience :
Non spécifiée
Administrative institution(s) :
CNRS
Université de Lille
Université de Lille
Research team(s) :
Computational Molecular Systems Biology
Submission date :
2020-02-12T15:11:21Z
2021-03-04T08:22:21Z
2021-03-04T08:22:21Z