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Pyran-containing sulfonamide hydroxamic acids: potent MMP inhibitors that spare MMP-1 |
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| Authors: | 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 |
| Affiliation: | Pfizer Global Research & Development, Groton Laboratories, Eastern Point Road, Groton, CT 06340, USA. reiterla@groton.pfizer.com |
| 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. |
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