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Literature DB >> 20837750

Antileishmanial and antitrypanosomal activities of the 8-aminoquinoline tafenoquine.

Vanessa Yardley¹, Francisco Gamarro, Simon L Croft.

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.

Entities: Chemical Disease Species

Mesh：

Substances：

Year: 2010 PMID： 20837750 PMCID： PMC2981226 DOI： 10.1128/AAC.00985-10

Source DB: PubMed Journal: Antimicrob Agents Chemother ISSN： 0066-4804 Impact factor: 5.191

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4. The Oral Antimalarial Drug Tafenoquine Shows Activity against Trypanosoma brucei.

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7. Evaluation of antimalarial activity and toxicity of a new primaquine prodrug.

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