The activity of diguanidino and 'reversed' diamidino 2,5-diarylfurans versus Trypanosoma cruzi and Leishmania donovani

Bioorg Med Chem Lett. 2003 Jun 16;13(12):2065-9. doi: 10.1016/s0960-894x(03)00319-6.

Abstract

The in vitro activity of 20 dicationic molecules containing either diguanidino or reversed amidine cationic groups were evaluated versus Trypanosoma cruzi and Leishmania donovani. The most active compounds were in the reversed amidine series and six exhibited IC(50) values of less than 1 micro mol versus T. cruzi and five gave similar values versus L. donovani.

Publication types

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

MeSH terms

  • Amidines / chemistry*
  • Amidines / pharmacology*
  • Animals
  • DNA / metabolism
  • Furans / chemistry*
  • Furans / pharmacology*
  • Guanidine / analogs & derivatives
  • Guanidine / pharmacology
  • Inhibitory Concentration 50
  • Leishmania donovani / cytology
  • Leishmania donovani / drug effects*
  • Leishmania donovani / metabolism
  • Macrophages / drug effects
  • Nucleic Acid Denaturation
  • Oligodeoxyribonucleotides / chemistry
  • Oligodeoxyribonucleotides / metabolism
  • Poly dA-dT / chemistry
  • Poly dA-dT / metabolism
  • Protozoan Proteins / antagonists & inhibitors
  • Structure-Activity Relationship
  • Temperature
  • Trypanocidal Agents / chemistry
  • Trypanocidal Agents / pharmacology
  • Trypanosoma cruzi / drug effects*
  • Trypanosoma cruzi / metabolism

Substances

  • Amidines
  • Furans
  • Oligodeoxyribonucleotides
  • Protozoan Proteins
  • Trypanocidal Agents
  • Poly dA-dT
  • DNA
  • Guanidine