Author/Authors :
Yue Mei Zhang، نويسنده , , Xiaodong Fan، نويسنده , , Devraj Chakaravarty، نويسنده , , Bangping Xiang، نويسنده , , Robert H. Scannevin، نويسنده , , Zhihong Huang، نويسنده , , Jianya Ma، نويسنده , , Sharon L. Burke، نويسنده , , Prabha Karnachi، نويسنده , , Kenneth J. Rhodes، نويسنده , , Paul F. Jackson، نويسنده ,
Abstract :
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.
Keywords :
1-Hydroxy-2-pyridone , Matrix metalloproteinase inhibitor , MMP-9 , stroke