title: From Dynamic Combinatorial Chemistry toin VivoEvaluation of Reversible and Irreversible Myeloperoxidase Inhibitors.
abstract: The implementation of dynamic combinatorial libraries allowed the determination of highly active reversible and irreversible inhibitors of myeloperoxidase (MPO) at the nanomolar level. Docking experiments highlighted the interaction between the most active ligands and MPO, and further kinetic studies defined the mode of inhibition of these compounds. Finally,in vivoevaluation showed that one dose of irreversible inhibitors is able to suppress the activity of MPO after inducing inflammation.
authors.affiliation: Chimie Pharmaceutique Organique, Faculty of pharmacy, Université Libre de Bruxelles (ULB) , Boulevard du Triomphe, 1050 Bruxelles, Belgium.
authors.forename: Jalal
authors.initials: J
authors.lastname: Soubhye
authors.affiliation: Chimie Pharmaceutique Organique, Faculty of pharmacy, Université Libre de Bruxelles (ULB) , Boulevard du Triomphe, 1050 Bruxelles, Belgium.
authors.forename: Michel
authors.initials: M
authors.lastname: Gelbcke
authors.affiliation: Chimie Pharmaceutique Organique, Faculty of pharmacy, Université Libre de Bruxelles (ULB) , Boulevard du Triomphe, 1050 Bruxelles, Belgium.
authors.forename: Pierre
authors.initials: P
authors.lastname: Van Antwerpen
authors.affiliation: Chimie Pharmaceutique Organique, Faculty of pharmacy, Université Libre de Bruxelles (ULB) , Boulevard du Triomphe, 1050 Bruxelles, Belgium.
authors.forename: François
authors.initials: F
authors.lastname: Dufrasne
authors.affiliation: Chimie Pharmaceutique Organique, Faculty of pharmacy, Université Libre de Bruxelles (ULB), Boulevard du Triomphe, 1050 Bruxelles, Belgium; Laboratory of Beneficial Microorganisms, Functional Food and Health (LMBAFS), Faculty of Natural Sciences and Life, Université de Abdelhamid Ibn Badis, 27000 Mostaganem, Algeria.
authors.forename: Mokhtaria Yasmina
authors.initials: MY
authors.lastname: Boufadi
authors.affiliation: Chimie Pharmaceutique Organique, Faculty of pharmacy, Université Libre de Bruxelles (ULB) , Boulevard du Triomphe, 1050 Bruxelles, Belgium.
authors.forename: Jean
authors.initials: J
authors.lastname: Nève
authors.affiliation: Department of Chemistry, BOKU-University of Natural Resources and Life Sciences , 1190 Vienna, Austria.
authors.forename: Paul G
authors.initials: PG
authors.lastname: Furtmüller
authors.affiliation: Department of Chemistry, BOKU-University of Natural Resources and Life Sciences , 1190 Vienna, Austria.
authors.forename: Christian
authors.initials: C
authors.lastname: Obinger
authors.affiliation: Laboratory of Experimental Medicine (ULB 222 unit), Université Libre de Bruxelles, Chu de Charleroi , 6110 Belgium.
authors.forename: Karim
authors.initials: K
authors.lastname: Zouaoui Boudjeltia
authors.affiliation: Laboratory of Biopolymers and Supramolecular Nanomaterials, Faculty of Pharmacy, Université Libre de Bruxelles (ULB) , Boulevard du Triomphe, 1050 Bruxelles, Belgium.
authors.forename: Franck
authors.initials: F
authors.lastname: Meyer
keywords: Myeloperoxidase; dynamic combinatorial chemistry; kinetic study; molecular docking; reversible and irreversible inhibitors