Antileishmanial and antitrypanosomal activities of the 8-aminoquinoline tafenoquine.
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.
Yardley
Vanessa
V
Faculty of Infectious and Tropical Disease, London School of Hygiene and Tropical Medicine, London WC1E 7HT, United Kingdom.yardley@lshtm.ac.uk
Gamarro
Francisco
F
Croft
Simon L
SL
D000634:Aminoquinolines / Q000494:pharmacology* / Q000627:therapeutic use; D000818:Animals; D000981:Antiprotozoal Agents / Q000494:pharmacology* / Q000627:therapeutic use; D005260:Female; D020128:Inhibitory Concentration 50; D007893:Leishmania donovani / Q000187:drug effects*; D007896:Leishmaniasis / Q000188:drug therapy / Q000469:parasitology; D008264:Macrophages / Q000469:parasitology*; D051379:Mice; D008807:Mice, Inbred BALB C; D011319:Primaquine / Q000494:pharmacology / Q000627:therapeutic use; D014349:Trypanosoma cruzi / Q000187:drug effects*
D000634:Aminoquinolines; D000981:Antiprotozoal Agents; C055852:tafenoquine; D011319:Primaquine; C080436:8-aminoquinoline