Title of article
Metabolism resistant isothiazolone inhibitors of cartilage breakdown Original Research Article
Author/Authors
Stephen W. Wright، نويسنده , , Joseph J. Petraitis، نويسنده , , Douglas G. Batt، نويسنده , , Ronald L. Corbett، نويسنده , , Susan V. Di Meo، نويسنده , , Bruce Freimark، نويسنده , , John V. Giannaras، نويسنده , , Michael J. Orwat، نويسنده , , Donald J. Pinto، نويسنده , , Michael A. Pratta، نويسنده , , Susan R. Sherk، نويسنده , , Herman F. Stampfli، نويسنده , , Jean M. Williams، نويسنده , , Ronald L. Magolda، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 1995
Pages
8
From page
227
To page
234
Abstract
A series of 2-(arylmethyl)pyridoisothiazolones is reported that inhibit the IL-1 β induced breakdown of bovine nasal septum cartilage in an organ culture assay. The synthesis and preliminary SAR of these compounds are described. These compounds represent a novel, non-peptide lead series approach to the mediation of the chronic cartilage breakdown associated with arthritic disease. These compounds are relatively resistant to reductive metabolism by liver microsomal preparations and appear to inhibit cartilage breakdown by interfering with the proteolytic activation of matrix metalloproteinases.
Journal title
Bioorganic and Medicinal Chemistry
Serial Year
1995
Journal title
Bioorganic and Medicinal Chemistry
Record number
1300421
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