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The discovery of a potent and selective lethal factor inhibitor for adjunct therapy of anthrax infection
Yusheng Xiong1, Judyann Wiltsie, Andrea Woods
1Merck Research laboratories, Rahway, NJ 07065, USA. yusheng.xiong@merck.com
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.
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