| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1365212 | Bioorganic & Medicinal Chemistry Letters | 2008 | 4 Pages |
Abstract
The structural features of an anthrax lethal factor inhibitor, N-oleoyldopamine (OLDA, 1) have been probed. The oleic acid moiety is critical, but, more interestingly, the presence of the double bond and its geometry were found to play an essential role. One compound, 5, was found to be an uncompetitive inhibitor of lethal factor (LF) with a Ki value of 2.2 μM and a cell-based IC50 value of 4.3 μM.
Graphical abstractThe structural features of an anthrax lethal factor inhibitor, N-oleoyldopamine (OLDA) have been probed. The oleic acid moiety is critical, but, more interestingly, the presence of the double bond and its geometry were found to play an essential role.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Brandon D. Gaddis, Charles M. Rubert Pérez, Jean Chmielewski,