| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1379262 | Bioorganic & Medicinal Chemistry Letters | 2006 | 5 Pages |
Abstract
A potent and selective anthrax LF inhibitor 40, (2R)-2-[(4-fluoro-3-methylphenyl)sulfonylamino]-N-hydroxy-2-(tetrahydro-2H-pyran-4-yl)acetamide, was identified through SAR study of a high throughput screen lead. It has an IC50 of 54 nM in the enzyme assay and an IC50 of 210 nM in the macrophage cytotoxicity assay. Compound 40 is also effective in vivo in several animal model studies.
Graphical abstractThis paper reports the synthesis and SAR of LF inhibitors. Compound 40 is potent against LF (IC50 54 nM) and efficacious in animals studies against anthrax spore challenges.Figure optionsDownload full-size imageDownload as PowerPoint slide
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Yusheng Xiong, Judyann Wiltsie, Andrea Woods, Jian Guo, James V. Pivnichny, Wei Tang, Alka Bansal, Richard T. Cummings, Barry R. Cunningham, Arthur M. Friedlander, Cameron M. Douglas, Scott P. Salowe, Dennis M. Zaller, Edward M. Scolnick,