Document Type

Article

Publication Date

10-2001

Publication Title

Bioorganic & Medicinal Chemistry Letters

Volume

11

Issue

20

Pages

2719-2722

Publisher Name

Elsevier

Abstract

A series of α-amino-β-sulphone hydroxamates was prepared and evaluated for potency versus MMP-13 and selectivity versus MMP-1. Various substituents were employed on the α-amino group (P1 position), as well as different groups attached to the sulphone group extending into P1′. Low nanomolar potency was obtained for MMP-13 with selectivity versus MMP-1 of >1000× for a number of analogues.

α-Amino-β-sulphone hydroxamates were prepared, which are potent MMP-13 inhibitors with selectivity versus MMP-1 of >1000× for a number of analogues. Selected compounds exhibited oral bioavailability.

Comments

Author Posting © Elsevier, 2001. This is the author's version of the work. It is posted here by permission of Elsevier for personal use, not for redistribution. The definitive version was published in Bioorganic & Medicinal Chemistry Letters, Volume 11, Issue 20, October 2001. https://doi.org/10.1016/S0960-894X(01)00556-X

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