| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1374273 | Bioorganic & Medicinal Chemistry Letters | 2010 | 4 Pages |
Abstract
Bacterial DNA gyrase is an attractive target for the investigation of new antibacterial agents. Inhibitors of the GyrB subunit, which contains the ATP-binding site, are described in this communication. Novel, substituted 5-(1H-pyrazol-3-yl)thiazole compounds were identified as inhibitors of bacterial gyrase. Structure-guided optimization led to greater enzymatic potency and moderate antibacterial potency. Data are presented for the demonstration of selective enzyme inhibition of Escherichia coli GyrB over Staphlococcus aureus GyrB.
Graphical abstractFigure optionsDownload full-size imageDownload as PowerPoint slide
Keywords
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Steven M. Ronkin, Michael Badia, Steve Bellon, Anne-Laure Grillot, Christian H. Gross, Trudy H. Grossman, Nagraj Mani, Jonathan D. Parsons, Dean Stamos, Martin Trudeau, Yunyi Wei, Paul S. Charifson,