title: Rapid discovery of potent α-fucosidase inhibitors by in situ screening of a library of (pyrrolidin-2-yl)triazoles.
abstract: The synthesis of a small library of (pyrrolidin-2-yl)triazoles via copper catalysed cycloaddition of an alkynyl iminocyclopentitol and a set of commercial and synthetic azides has been achieved. The in situ screening for the activity towards α-fucosidase of the resulting triazoles has allowed the identification of one of the most potent and selective pyrrolidine derived inhibitors of this enzyme (Ki = 4 nM).
authors.affiliation: Department of Organic Chemistry, Faculty of Chemistry, University of Seville, C/Prof. García González, 1, 41012-Seville, Spain. ajmoreno@us.es.
authors.forename: Pilar
authors.initials: P
authors.lastname: Elías-Rodríguez
authors.forename: Elena
authors.initials: E
authors.lastname: Moreno-Clavijo
authors.forename: Ana T
authors.initials: AT
authors.lastname: Carmona
authors.forename: Antonio J
authors.initials: AJ
authors.lastname: Moreno-Vargas
authors.forename: Inmaculada
authors.initials: I
authors.lastname: Robina
mesh_terms: D000818:Animals; D002417:Cattle; D055808:Drug Discovery; D004353:Drug Evaluation, Preclinical; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D006863:Hydrogen-Ion Concentration; D007668:Kidney / Q000201:enzymology; D054852:Small Molecule Libraries / Q000032:analysis* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D014230:Triazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D005644:alpha-L-Fucosidase / Q000037:antagonists & inhibitors* / Q000378:metabolism
chemical_list: D004791:Enzyme Inhibitors; D054852:Small Molecule Libraries; D014230:Triazoles; D005644:alpha-L-Fucosidase