Journal
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
Volume 54, Issue 12, Pages 5356-5358Publisher
AMER SOC MICROBIOLOGY
DOI: 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 mu M for both pentavalent antimony (SbV)-sensitive and SbV-resistant strains and by oral administration in BALB/c mice, with 50% effective dose (ED50) values of 1.2 to 3.5 mg/kg for 5 days. Tafenoquine was less active against intracellular Trypanosoma cruzi amastigotes, with an IC50 of 21.9 mu M.
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