815576-04-6Relevant articles and documents
Pyran-containing sulfonamide hydroxamic acids: Potent MMP inhibitors that spare MMP-1
Reiter, Lawrence A.,Robinson, Ralph P.,McClure, Kim F.,Jones, Christopher S.,Reese, Matthew R.,Mitchell, Peter G.,Otterness, Ivan G.,Bliven, Marcia L.,Liras, Jennifer,Cortina, Santo R.,Donahue, Kathleen M.,Eskra, James D.,Griffiths, Richard J.,Lame, Mary E.,Lopez-Anaya, Arturo,Martinelli, Gary J.,McGahee, Shunda M.,Yocum, Sue A.,Lopresti-Morrow, Lori L.,Tobiassen, Lisa M.,Vaughn-Bowser, Marcie L.
, p. 3389 - 3395 (2004)
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.
