Phosphonium lipocations as antiparasitic agents

Bioorg Med Chem Lett. 2012 Apr 15;22(8):2976-9. doi: 10.1016/j.bmcl.2012.02.045. Epub 2012 Feb 23.

Abstract

Phosphonium lipocations were synthesized and evaluated for inhibition of the development of Plasmodium falciparum and Trypanosoma cruzi, etiological agents of malaria and Chagas disease, respectively. Optimal phthalimides and 1,4-naphthoquinone-based lipocations were active in vitro at mid-high nM concentrations against P. falciparum and low μM concentrations against T. cruzi.

Publication types

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

MeSH terms

  • Animals
  • Antiparasitic Agents / chemistry*
  • Antiparasitic Agents / pharmacokinetics
  • Antiparasitic Agents / pharmacology*
  • Cations
  • Chagas Disease / drug therapy
  • Chlorocebus aethiops
  • Humans
  • Inhibitory Concentration 50
  • Lipids / chemistry
  • Lipids / pharmacokinetics
  • Models, Biological
  • Organophosphorus Compounds / chemistry
  • Organophosphorus Compounds / pharmacokinetics
  • Organophosphorus Compounds / pharmacology
  • Plasmodium falciparum / drug effects*
  • Trypanosoma cruzi / drug effects*
  • Ubiquinone / analogs & derivatives
  • Ubiquinone / chemistry
  • Ubiquinone / pharmacokinetics
  • Ubiquinone / pharmacology
  • Vero Cells

Substances

  • Antiparasitic Agents
  • Cations
  • Lipids
  • Organophosphorus Compounds
  • Ubiquinone
  • mitoquinone