Title of article :
Design, synthesis, and structural analysis of inhibitors of influenza neuraminidase containing a 2,3-disubstituted tetrahydrofuran-5-carboxylic acid core
Author/Authors :
Gary T. Wang، نويسنده , , Sheldon Wang، نويسنده , , Robert Gentles، نويسنده , , Thomas Sowin، نويسنده , , Clarence J. Maring، نويسنده , , Dale J. Kempf، نويسنده , , Warren M. Kati، نويسنده , , Vincent Stoll، نويسنده , , Kent D. Stewart، نويسنده , , W. Graeme Laver، نويسنده ,
Abstract :
(±)-(2R,3R,5R)-[2-(1′-S-Acetamido-3′-methyl)butyl-3-methoxycarbonyl]tetrahydrofuran-5-carboxylic acid (9) and (±)-(2R,3R,5R)-[2-(1′-S-acetamido-3′-methyl)butyl-3-(4′-imidazolyl)]tetrahydrofuran 5-carboxylic acid (14) were synthesized as inhibitors of influenza neuraminidase (NA). Both compounds 9 and 14 inhibit influenza NA A with an IC50 of about 0.5 μM and NA B with an IC50 of 1.0 μM.
