Author/Authors :
Shyh-Ming Yang، نويسنده , , Robert H. Scannevin، نويسنده , , Bingbing Wang، نويسنده , , Sharon L. Burke، نويسنده , , Zhihong Huang، نويسنده , , Prabha Karnachi، نويسنده , , Lawrence J. Wilson، نويسنده , , Kenneth J. Rhodes، نويسنده , , Bharat Lagu، نويسنده , , William V. Murray، نويسنده ,
Abstract :
The introduction and the optimization of an α-amino substituent based on a series of α-hydroxy-β-N-biaryl ether sulfonamide hydroxamates is described. The modification leads to a new series of MMP-2/MMP-9 inhibitors with enhanced inhibitory activities and improved ADME properties. An efficacy study on reducing the ischemia-induced brain edema in the rat transient middle cerebral artery occlusion (tMCAo) model is also demonstrated.
Keywords :
Gelatinase , matrix metalloproteinase , MMP inhibitor , Hydroxamate , stroke
