• Publications
  • Influence
Pyran-containing sulfonamide hydroxamic acids: potent MMP inhibitors that spare MMP-1.
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. TheExpand
  • 46
  • 3
Potent, selective pyrimidinetrione-based inhibitors of MMP-13.
Using SAR from two related series of pyrimidinetrione-based inhibitors, compounds with potent MMP-13 inhibition and >100-fold selectivity against other MMPs have been identified. Despite highExpand
  • 42
  • 3
  • PDF
The preclinical pharmacological profile of the potent and selective leukotriene B4 antagonist CP-195543.
CP-195543 [(+)-2-(3-benzyl-4-hydroxy-chroman-7-yl)-4-trifluoromethyl-benzoic acid] is a structurally novel, selective and potent leukotriene B4 (LTB4) receptor antagonist. In vitro CP-195543Expand
  • 45
  • 2
Phosphinic acid-based MMP-13 inhibitors that spare MMP-1 and MMP-3.
Phosphinic acid-based inhibitors of MMP-13 have been investigated with the aim of identifying potent inhibitors with high selectivity versus MMP-1. Independent variation of the substituents on aExpand
  • 30
  • 2
Inhibition of MMP-1 and MMP-13 with phosphinic acids that exploit binding in the S2 pocket.
Through the use of empirical and computational methods, phosphinate-based inhibitors of MMP-1 and MMP-13 that bind into the S2 pocket of these enzymes were designed. The synthesis and testing of 2Expand
  • 21
  • 2
Potent pyrimidinetrione-based inhibitors of MMP-13 with enhanced selectivity over MMP-14.
Through the use of computational modeling, a series of pyrimidinetrione-based inhibitors of MMP-13 was designed based on a lead inhibitor identified through file screening. Incorporation of a biarylExpand
  • 41
  • 1
Potent, selective spiropyrrolidine pyrimidinetrione inhibitors of MMP-13.
Explorations in the pyrimidinetrione series of MMP-13 inhibitors led to the discovery of a series of spiro-fused compounds that are potent and selective inhibitors of MMP-13. While other spiro-fusedExpand
  • 19
  • 1
Inhibition of Interleukin‐1—Stimulated Collagen Degradation in Cartilage Explants
One of the characteristics of joint diseases such as osteoarthritis is a progressive loss of matrix constituents, leading to fibrillation and thinning of the articular cartilage. Members of theExpand
  • 2
  • 1