β-N-Biaryl ether sulfonamide hydroxamates as potent gelatinase inhibitors: Part 2. Optimization of α-amino substituents

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.

A new series of α-amino-β-N-biaryl ether sulfonamide hydroxamates as potent gelatinase inhibitors is described.Figure optionsDownload as PowerPoint slide