Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10591918 | Bioorganic & Medicinal Chemistry Letters | 2013 | 13 Pages |
Abstract
A novel series of non-nucleoside thumb pocket 2 HCV NS5B polymerase inhibitors were derived from a fragment-based approach using information from X-ray crystallographic analysis of NS5B-inhibitor complexes and iterative rounds of parallel synthesis. Structure-based drug design strategies led to the discovery of potent sub-micromolar inhibitors 11a-c and 12a-c from a weak-binding fragment-like structure 1 as a starting point.
Keywords
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Timothy A. Stammers, René Coulombe, Jean Rancourt, Bounkham Thavonekham, Gulrez Fazal, Sylvie Goulet, Araz Jakalian, Dominic Wernic, Youla Tsantrizos, Marc-André Poupart, Michael Bös, Ginette McKercher, Louise Thauvette, George Kukolj,