Potent second generation vinyl sulfonamide inhibitors of the trypanosomal cysteine protease cruzain

Bioorg Med Chem Lett. 2001 Oct 22;11(20):2759-62. doi: 10.1016/s0960-894x(01)00566-2.

Abstract

A new family of potent N-alkoxyvinylsulfonamide inhibitors of cruzain have been developed. Inhibitor 13 has a second order inactivation rate constant of 6,480,000s(-1)M(-1) versus cruzain, and is also highly effective against Trypanosoma cruzi trypomastigotes in a tissue culture assay.

Publication types

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

MeSH terms

  • Animals
  • Cysteine Endopeptidases / metabolism
  • Cysteine Proteinase Inhibitors / chemical synthesis*
  • Cysteine Proteinase Inhibitors / chemistry
  • Cysteine Proteinase Inhibitors / pharmacology
  • Parasitic Sensitivity Tests
  • Protozoan Proteins / antagonists & inhibitors*
  • Protozoan Proteins / metabolism
  • Sulfonamides / chemical synthesis*
  • Sulfonamides / chemistry
  • Sulfonamides / pharmacology*
  • Trypanocidal Agents / chemical synthesis*
  • Trypanocidal Agents / chemistry
  • Trypanocidal Agents / pharmacology
  • Trypanosoma cruzi / drug effects*

Substances

  • Cysteine Proteinase Inhibitors
  • Protozoan Proteins
  • Sulfonamides
  • Trypanocidal Agents
  • vinyl sulfonamide
  • Cysteine Endopeptidases
  • cruzain, Trypanosoma cruzi