Dipeptidyl-alpha,beta-epoxyesters as potent irreversible inhibitors of the cysteine proteases cruzain and rhodesain

Bioorg Med Chem Lett. 2007 Dec 15;17(24):6697-700. doi: 10.1016/j.bmcl.2007.10.056. Epub 2007 Oct 22.

Abstract

The dipeptidyl epoxyesters 3 and 4 are potent, irreversible inhibitors of cruzain and rhodesain.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cysteine Endopeptidases / metabolism*
  • Cysteine Proteinase Inhibitors / chemical synthesis*
  • Cysteine Proteinase Inhibitors / chemistry
  • Cysteine Proteinase Inhibitors / pharmacology*
  • Dipeptides / chemistry*
  • Epoxy Compounds / chemistry*
  • Esters / chemical synthesis*
  • Esters / chemistry
  • Esters / pharmacology*
  • Inhibitory Concentration 50
  • Molecular Structure
  • Stereoisomerism
  • Trypanosoma brucei brucei / drug effects

Substances

  • Cysteine Proteinase Inhibitors
  • Dipeptides
  • Epoxy Compounds
  • Esters
  • Cysteine Endopeptidases