Novel, potent, selective, and orally bioavailable human betaII-tryptase inhibitors

Bioorg Med Chem Lett. 2006 Aug 1;16(15):4085-9. doi: 10.1016/j.bmcl.2006.04.088. Epub 2006 May 24.

Abstract

The synthesis of novel [1,2,4]oxadiazoles and their structure-activity relationship (SAR) for the inhibition of tryptase and related serine proteases is presented. Elaboration of the P'-side afforded potent, selective, and orally bioavailable tryptase inhibitors.

MeSH terms

  • Administration, Oral
  • Biological Availability
  • Enzyme Inhibitors / administration & dosage
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / pharmacology*
  • Models, Molecular
  • Serine Endopeptidases / drug effects*
  • Structure-Activity Relationship
  • Tryptases

Substances

  • Enzyme Inhibitors
  • Serine Endopeptidases
  • Tryptases