Acyl dipeptides as reversible caspase inhibitors. Part 1: initial lead optimization

Bioorg Med Chem Lett. 2002 Oct 21;12(20):2969-71. doi: 10.1016/s0960-894x(02)00629-7.

Abstract

Parallel synthesis was used to explore the SAR of a peptidomimetic caspase inhibitor. The most potent compound had nanomolar activity against caspases 1, 3, 6, 7, and 8.

MeSH terms

  • Acylation
  • Caspase Inhibitors*
  • Dipeptides / chemical synthesis*
  • Dipeptides / pharmacology*
  • Enzyme Inhibitors / chemical synthesis*
  • Enzyme Inhibitors / pharmacology*
  • Indicators and Reagents
  • Isoenzymes / antagonists & inhibitors
  • Oligopeptides / chemical synthesis
  • Oligopeptides / pharmacology
  • Structure-Activity Relationship

Substances

  • Caspase Inhibitors
  • Dipeptides
  • Enzyme Inhibitors
  • Indicators and Reagents
  • Isoenzymes
  • Oligopeptides