Activity of diimidazoline amides against African trypanosomiasis

Bioorg Med Chem Lett. 2014 Feb 1;24(3):944-8. doi: 10.1016/j.bmcl.2013.12.064. Epub 2013 Dec 22.

Abstract

We identified several diimidazoline mono- and diamides that were as potent as pentamidine against Trypanosoma brucei rhodesiense in vitro. All of these were also less cytotoxic than pentamidine, but none was as effective as the latter in a T. brucei rhodesiense-infected mouse model. A single imidazoline may be sufficient for high antitrypanosomal activity provided that a second weak base functional group is present.

Keywords: African trypanosomiasis; Diimidazoline; Trypanosoma brucei rhodesiense.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amides / chemistry
  • Amides / pharmacology*
  • Amides / therapeutic use
  • Animals
  • Disease Models, Animal
  • Humans
  • Imidazolines / chemistry
  • Imidazolines / therapeutic use*
  • Mice
  • Molecular Structure
  • Trypanocidal Agents / chemistry*
  • Trypanocidal Agents / pharmacology*
  • Trypanosoma / drug effects*
  • Trypanosomiasis, African / drug therapy

Substances

  • Amides
  • Imidazolines
  • Trypanocidal Agents