Inhibitors of anthrax lethal factor

An inhibitor of anthrax lethal toxin mediated cell death (1) was identified by a medium throughput cell-based screen. This compound was determined to specifically inhibit anthrax lethal factor (LF), and subsequent SAR studies produced an even more potent inhibitor (4). Mechanistic studies identified these agents as uncompetitive inhibitors of LF with Ki values of 3.0 and 1.7 μM, respectively, with good cell potency and low cytotoxicity.

Graphical abstractAn inhibitor of anthrax lethal factor (1) was discovered. A subsequent SAR and mechanistic study was performed to identify uncompetitive inhibitors of anthrax lethal factor with good cell potency and low cytotoxicity.Figure optionsDownload full-size imageDownload as PowerPoint slide