| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1372062 | Bioorganic & Medicinal Chemistry Letters | 2010 | 5 Pages |
Inactivators of plasminogen activator inhibitor-1 (PAI-1) have been identified as possible treatments for a range of conditions, including atherosclerosis, venous thrombosis, and obesity. We describe the synthesis and inhibitory activity of a novel series of compounds based on bis-arylsulfonamide and aryl sulfonimide motifs that show potent and specific activity towards PAI-1. Inhibitors containing short linking units between the sulfonyl moieties and a 3,4-dihydroxy aryl substitution pattern showed the most potent inhibitory activity, and retained high specificity for PAI-1 over the structurally-related serpin anti-thrombin III (ATIII).
Graphical abstractThe synthesis and evaluation of potent and novel bis-arylsulfonamide and arylsulfonimide-based inhibitors of plasminogen activator inhibitor-1 (PAI-1) is described.Figure optionsDownload full-size imageDownload as PowerPoint slide
