Author(s): Reiter LA, Robinson RP, McClure KF, Jones CS, Reese MR,
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Abstract The SAR of a series of sterically hindered sulfonamide hydroxamic acids with relatively large P1' 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.
This article was published in Bioorg Med Chem Lett
and referenced in Medicinal Chemistry