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

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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.

α-Alkyl-α-amino-β-sulphone hydroxamates were prepared, which are potent MMP-2 and MMP-13 inhibitors with selectivity versus MMP-1 ranging from >10 to >1000. Selected compounds were orally bioavailable.

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