Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1366974 | Bioorganic & Medicinal Chemistry Letters | 2007 | 5 Pages |
Abstract
Two sets of five thioimidoyl α-l-arabino- and β-d-galactofuranosides were designed, synthesized and subjected to docking studies to evaluate their ability to be recognized by the active site of the α-l-arabinofuranosidase AbfD3. Further in vitro assays showed that the targeted furanosides are the first potent inhibitors of this furanosyl hydrolase and that the most efficient one, the thiazolyl α-l-arabinofuranoside 1, is a competitive inhibitor having a KI of 1.4 μM.
Graphical abstractThe synthesis and in vitro activity of the powerful furanosidic inhibitors of the arabinofuranosidase AbfD3 are reported.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Gérald Lopez, Richard Daniellou, Michael O’Donohue, Vincent Ferrières, Caroline Nugier-Chauvin,