Title of article :
Design, synthesis, and neuraminidase inhibitory activity of GS-4071 analogues that utilize a novel hydrophobic paradigm
Author/Authors :
Stephen Hanessian، نويسنده , , Jianchio Wang، نويسنده , , Debra Montgomery، نويسنده , , Vincent Stoll، نويسنده , , Kent D. Stewart، نويسنده , , Warren Kati، نويسنده , , Clarence Maring، نويسنده , , Dale Kempf، نويسنده , , Charles Hutchins، نويسنده , , W. Graeme Laver، نويسنده ,
Abstract :
Structure-based design has led to the synthesis of a novel analogue of GS-4071, an influenza neuraminidase inhibitor, in which the basic amino group has been replaced by a hydrophobic vinyl group. An X-ray co-crystal structure of the new inhibitor (Ki=45 nM) bound to the active site shows that the vinyl group occupies the same subsite as the amino group in GS-4071.
