Antileishmanial and antitrypanosomal activities of the 8-aminoquinoline tafenoquine.
Yardley, Vanessa;
Gamarro, Francisco;
Croft, Simon L;
(2010)
Antileishmanial and antitrypanosomal activities of the 8-aminoquinoline tafenoquine.
Antimicrobial agents and chemotherapy, 54 (12).
pp. 5356-5358.
ISSN 0066-4804
DOI: https://doi.org/10.1128/AAC.00985-10
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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.
