Design, synthesis and biological evaluation of succinimide derivatives as potential mechanism-based inhibitors of human leukocyte elastase, cathepsin G and proteinase 3

Bioorg Med Chem. 1995 Apr;3(4):375-81. doi: 10.1016/0968-0896(95)00024-b.

Abstract

Structure-activity relationship study and in vitro biochemical studies with human leukocyte elastase, cathepsin G and proteinase 3 were conducted using a series of succinimide derivatives.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Amino Acids / chemistry
  • Cathepsin G
  • Cathepsins / antagonists & inhibitors*
  • Drug Design
  • Enzyme Inhibitors / chemical synthesis
  • Enzyme Inhibitors / chemistry*
  • Enzyme Inhibitors / pharmacology*
  • Humans
  • Leukocyte Elastase
  • Myeloblastin
  • Pancreatic Elastase / antagonists & inhibitors*
  • Serine Endopeptidases / drug effects*
  • Serine Proteinase Inhibitors / pharmacology*
  • Structure-Activity Relationship
  • Succinimides / chemical synthesis
  • Succinimides / chemistry*
  • Succinimides / pharmacology*
  • Time Factors

Substances

  • Amino Acids
  • Enzyme Inhibitors
  • Serine Proteinase Inhibitors
  • Succinimides
  • succinimide
  • Cathepsins
  • Serine Endopeptidases
  • CTSG protein, human
  • Cathepsin G
  • Pancreatic Elastase
  • Leukocyte Elastase
  • Myeloblastin