5,5-Fused thiophene gamma-lactams as templates for serine protease inhibition

Chem Commun (Camb). 2002 Jun 21:(12):1274-5. doi: 10.1039/b111627d.

Abstract

Novel 5,5-fused thiophene lactams are potent inhibitors and acylating agents of HNE and PPE.

MeSH terms

  • Alkylating Agents / chemical synthesis
  • Animals
  • Binding Sites
  • Crystallography, X-Ray
  • Humans
  • Lactams / chemical synthesis*
  • Leukocyte Elastase / antagonists & inhibitors
  • Mass Spectrometry
  • Molecular Conformation
  • Pancreatic Elastase / antagonists & inhibitors
  • Serine Proteinase Inhibitors / chemical synthesis*
  • Swine
  • Thiophenes / chemical synthesis*

Substances

  • Alkylating Agents
  • Lactams
  • Serine Proteinase Inhibitors
  • Thiophenes
  • Pancreatic Elastase
  • Leukocyte Elastase