Jump to main content
Jump to site search

Issue 31, 2014
Previous Article Next Article

Rapid discovery of potent α-fucosidase inhibitors by in situ screening of a library of (pyrrolidin-2-yl)triazoles

Author affiliations

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).

Graphical abstract: Rapid discovery of potent α-fucosidase inhibitors by in situ screening of a library of (pyrrolidin-2-yl)triazoles

Back to tab navigation

Supplementary files

Article information


Submitted
06 May 2014
Accepted
12 Jun 2014
First published
12 Jun 2014

Org. Biomol. Chem., 2014,12, 5898-5904
Article type
Paper
Author version available

Rapid discovery of potent α-fucosidase inhibitors by in situ screening of a library of (pyrrolidin-2-yl)triazoles

P. Elías-Rodríguez, E. Moreno-Clavijo, A. T. Carmona, A. J. Moreno-Vargas and I. Robina, Org. Biomol. Chem., 2014, 12, 5898
DOI: 10.1039/C4OB00931B

Social activity

Search articles by author

Spotlight

Advertisements