α-Alkyl-α-amino-β-sulphone hydroxamates as potent MMP inhibitors that spare MMP-1

…, G DeCrescenzo, J Freskos, DP Getman…

Index: Becker, Daniel P; DeCrescenzo, Gary; Freskos, John; Getman, Daniel P; Hockerman, Susan L; Li, Madeleine; Mehta, Pramod; Munie, Grace E; Swearingen, Craig Bioorganic and Medicinal Chemistry Letters, 2001 , vol. 11, # 20 p. 2723 - 2725

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Citation Number: 26

Abstract

A series of α-alkyl-α-amino-β-sulphone hydroxamates was prepared and evaluated for potency versus MMP-2 and MMP-13, and for selectivity versus MMP-1. Low nanomolar potency was obtained with selectivity versus MMP-1 ranging from> 10 to> 1000. Selected compounds were orally bioavailable.