Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1376950 | Bioorganic & Medicinal Chemistry Letters | 2008 | 5 Pages |
Matrix metalloproteinase-9 (MMP-9) has been implicated in the breakdown of the blood–brain barrier during cerebral ischemia. As a result, inhibition of MMP-9 may have utility as a therapeutic intervention in stroke. Towards this end, we have synthesized a series of 1-hydroxy-2-pyridinones that have excellent in vitro potency in inhibiting MMP-9 in addition to MMP-2. Representative compounds also demonstrate good efficacy in the mouse transient mid-cerebral artery occlusion (tMCAO) model of cerebral ischemia.
Graphical abstractA series of 1-hydroxy-2-pyridinone synthesized have excellent in vitro potency in inhibiting MMP-9 in addition to MMP-2 and representative compounds demonstrate good efficacy in the mouse transient mid-cerebral artery occlusion (tMCAO) model of cerebral ischemia.Figure optionsDownload full-size imageDownload as PowerPoint slide