The discovery of a potent and selective lethal factor inhibitor for adjunct therapy of anthrax infection.

Bioorg Med Chem Lett

Authors	Yusheng Xiong Judyann Wiltsie Andrea Woods Jian Guo James Pivnichny Wei Tang Alka Bansal Richard Cummings Barry Cunningham Arthur Friedlander Cameron Douglas Scott Salowe Dennis Zaller Edward Scolnick Dennis Schmatz Kenneth Bartizal Jeffrey Hermes Malcolm MacCoss Kevin Chapman
Keywords	Animals Mice Dogs Antigens, Bacterial Bacterial Toxins Rabbits Structure-Activity Relationship Macaca mulatta Molecular Structure Drug Evaluation, Preclinical Stereoisomerism Pyrans Anthrax Biological Availability Metalloproteases
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.
Year of Publication	2006
Journal	Bioorg Med Chem Lett
Volume	16
Issue	4
Pages	964-8
Date Published	2006 Feb 15
ISSN	0960-894X
DOI	10.1016/j.bmcl.2005.10.088
PubMed ID	16338135
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