alpha-amino-beta-sulphone hydroxamates as potent MMP-13 inhibitors that spare MMP-1

Authors
Becker, DP Barta, TE Bedell, L DeCrescenzo, G Freskos, J Getman, DP Hockerman, SL Li, M Mehta, P Mischke, B Munie, GE Swearingen, C Villamil, CL
Citation
Dp. Becker et al., alpha-amino-beta-sulphone hydroxamates as potent MMP-13 inhibitors that spare MMP-1, BIOORG MED, 11(20), 2001, pp. 2719-2722
Citations number
21
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
20
Year of publication
2001
Pages
2719 - 2722
Database
ISI
SICI code
0960-894X(20011022)11:20<2719:AHAPMI>2.0.ZU;2-I
Abstract
A series of alpha -amino-beta -sulphone hydroxamates was prepared and evalu ated for potency versus MMP-13 and selectivity versus MMP-1. Various substi tuents were employed on the alpha -amino group (P-1 position), as well as d ifferent groups attached to the sulphone group extending into P-1'. Low nan omolar potency was obtained for MMP-13 with selectivity versus MMP-1 of > 1 000x for a number of analogues. (C) 2001 Elsevier Science Ltd. All rights r eserved.