| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1371687 | Bioorganic & Medicinal Chemistry Letters | 2012 | 5 Pages |
Abstract
Four core structures capable of providing sub-nanomolar inhibitors of anthrax lethal factor (LF) were evaluated by comparing the potential for toxicity, physicochemical properties, in vitro ADME profiles, and relative efficacy in a rat lethal toxin (LT) model of LF intoxication. Poor efficacy in the rat LT model exhibited by the phenoxyacetic acid series (3) correlated with low rat microsome and plasma stability. Specific molecular interactions contributing to the high affinity of inhibitors with a secondary amine in the C2-side chain were revealed by X-ray crystallography.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Guan-Sheng Jiao, Seongjin Kim, Mahtab Moayeri, Devorah Crown, April Thai, Lynne Cregar-Hernandez, Linda McKasson, Banumathi Sankaran, Axel Lehrer, Teri Wong, Lisa Johns, Stephen A. Margosiak, Stephen H. Leppla, Alan T. Johnson,