Second generation of thiazolylmannosides, FimH antagonists for E. coli-induced Crohn's disease - INRAE - Institut national de recherche pour l’agriculture, l’alimentation et l’environnement Accéder directement au contenu
Article Dans Une Revue Organic & Biomolecular Chemistry Année : 2016

Second generation of thiazolylmannosides, FimH antagonists for E. coli-induced Crohn's disease

Résumé

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.
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Dates et versions

hal-02077029 , version 1 (22-03-2019)

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Citer

T. Chalopin, D. Alvarez Dorta, Adeline Sivignon, M. Caudan, T. Dumych, et al.. Second generation of thiazolylmannosides, FimH antagonists for E. coli-induced Crohn's disease. Organic & Biomolecular Chemistry, 2016, 14 (16), pp.3913-3925. ⟨10.1039/c6ob00424e⟩. ⟨hal-02077029⟩
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