Article ID Journal Published Year Pages File Type
1377359 Bioorganic & Medicinal Chemistry Letters 2008 6 Pages PDF
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.

Graphical abstractA new series of α-amino-β-N-biaryl ether sulfonamide hydroxamates as potent gelatinase inhibitors is described.Figure optionsDownload full-size imageDownload as PowerPoint slide

Related Topics
Physical Sciences and Engineering Chemistry Organic Chemistry
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