Potent, selective spiropyrrolidine pyrimidinetrione inhibitors of MMP-13

Bioorg Med Chem Lett. 2007 Dec 1;17(23):6529-34. doi: 10.1016/j.bmcl.2007.09.085. Epub 2007 Sep 29.

Abstract

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-fused motifs are hydrolytically unstable, presumably due to electronic destabilization of the pyrimidinetrione ring, the spiropyrrolidine series does not share this liability. Greater than 100-fold selectivity versus other MMP family members was achieved by incorporation of an extended aryl-heteroaryl P1'group. When dosed as the sodium salt, these compounds displayed excellent oral absorption and pharmacokinetic properties. Despite the selectivity, a representative of this series produced fibroplasia in a 14 day rat study.

Publication types

  • Comparative Study

MeSH terms

  • Animals
  • Enzyme Stability / drug effects
  • Matrix Metalloproteinase 13 / metabolism
  • Matrix Metalloproteinase Inhibitors*
  • Protease Inhibitors / chemistry*
  • Protease Inhibitors / pharmacology
  • Pyrimidines / chemistry*
  • Pyrimidines / pharmacology
  • Pyrrolidines / chemistry*
  • Pyrrolidines / pharmacology
  • Rats
  • Spiro Compounds / chemistry*
  • Spiro Compounds / pharmacology
  • Structure-Activity Relationship

Substances

  • Matrix Metalloproteinase Inhibitors
  • Protease Inhibitors
  • Pyrimidines
  • Pyrrolidines
  • Spiro Compounds
  • Matrix Metalloproteinase 13