Title of article
α-Amino-β-sulphone hydroxamates as potent MMP-13 inhibitors that spare MMP-1
Author/Authors
Daniel P. Becker، نويسنده , , Thomas E. Barta، نويسنده , , Louis Bedell، نويسنده , , Gary DeCrescenzo، نويسنده , , John Freskos، نويسنده , , Daniel P. Getman، نويسنده , , Susan L. Hockerman، نويسنده , , Madeleine Li، نويسنده , , Pramod Mehta، نويسنده , , Brent Mischke، نويسنده , , Grace E. Munie، نويسنده , , Craig Swearingen، نويسنده , , Clara I. Villamil، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2001
Pages
4
From page
2719
To page
2722
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.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2001
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
791715
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