Pyran-containing sulfonamide hydroxamic acids: potent MMP inhibitors that spare MMP-1
Graphic The SAR of a series of sterically hindered sulfonamide hydroxamic acids with relatively large P 1′ groups is described. The compounds typically spare MMP-1 while being potent inhibitors of MMP-13. The metabolically more stable compounds in the series contain either a monocyclic or bicyclic p...
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Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2004-07, Vol.14 (13), p.3389-3395 |
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Hauptverfasser: | , , , , , , , , , , , , , , , , , , , , |
Format: | Artikel |
Sprache: | eng |
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Zusammenfassung: | Graphic
The SAR of a series of sterically hindered sulfonamide hydroxamic acids with relatively large P
1′ groups is described. The compounds typically spare MMP-1 while being potent inhibitors of MMP-13. The metabolically more stable compounds in the series contain either a monocyclic or bicyclic pyran ring adjacent to the hydroxamate group. Despite the sparing of MMP-1, pre-clinical and clinical studies revealed that fibrosis in rats and MSS in humans is still produced. |
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ISSN: | 0960-894X 1464-3405 |
DOI: | 10.1016/j.bmcl.2004.04.083 |