| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1379060 | Bioorganic & Medicinal Chemistry Letters | 2006 | 5 Pages |
Anthrax lethal factor is a Zn2+-dependent metalloprotease and the key virulence factor of tripartite anthrax toxin secreted by Bacillus anthracis, the causative agent of anthrax. A series of guanidinylated 2,5-dideoxystreptamine derivatives were designed and synthesized as inhibitors of lethal factor, some of which show strong inhibitory activity against lethal factor in an in vitro FRET assay. Preparation and structure–activity relationships of these compounds are presented.
Graphical abstractAnthrax lethal factor is a Zn2+-dependent metalloprotease and the key virulence factor of tripartite anthrax toxin secreted by Bacillus anthracis, the causative agent of anthrax. A series of guanidinylated 2,5-dideoxystreptamine derivatives were designed and synthesized as inhibitors of lethal factor, some of which show strong inhibitory activity against lethal factor in an in vitro FRET assay. Preparation and structure–activity relationships of these compounds are presented.Figure optionsDownload full-size imageDownload as PowerPoint slide
