Antileishmanial and antitrypanosomal activities of the 8-aminoquinoline tafenoquine

Antimicrob Agents Chemother. 2010 Dec;54(12):5356-8. doi: 10.1128/AAC.00985-10. Epub 2010 Sep 13.

Abstract

The 8-aminoquinoline tafenoquine showed significant in vitro activity against Leishmania species, including L. donovani amastigotes in macrophages, with 50% inhibitory concentrations (IC(50)s) between 0.1 and 4.0 μM for both pentavalent antimony (SbV)-sensitive and SbV-resistant strains and by oral administration in BALB/c mice, with 50% effective dose (ED(50)) values of 1.2 to 3.5 mg/kg for 5 days. Tafenoquine was less active against intracellular Trypanosoma cruzi amastigotes, with an IC(50) of 21.9 μM.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aminoquinolines / pharmacology*
  • Aminoquinolines / therapeutic use
  • Animals
  • Antiprotozoal Agents / pharmacology*
  • Antiprotozoal Agents / therapeutic use
  • Female
  • Inhibitory Concentration 50
  • Leishmania donovani / drug effects*
  • Leishmaniasis / drug therapy
  • Leishmaniasis / parasitology
  • Macrophages / parasitology*
  • Mice
  • Mice, Inbred BALB C
  • Primaquine / pharmacology
  • Primaquine / therapeutic use
  • Trypanosoma cruzi / drug effects*

Substances

  • Aminoquinolines
  • Antiprotozoal Agents
  • tafenoquine
  • Primaquine
  • 8-aminoquinoline