Evaluation of α,β-unsaturated ketones as antileishmanial agents

Miguel A. Vasquez, Eva Iniguez, Umashankar Das, Stephen M. Beverley, Linda J. Herrera, Jonathan R. Dimmock, Rosa A. Maldonado

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Abstract

In this study, we assessed the antileishmanial activity of 126 α,β-unsaturated ketones. The compounds NC901, NC884, and NC2459 showed high leishmanicidal activity for both the extracellular (50% effective concentration [EC50], 456 nM, 1,122 nM, and 20 nM, respectively) and intracellular (EC50, 1,870 nM, 937 nM, and 625 nM, respectively) forms of Leishmania major propagated in macrophages, with little or no toxicity to mammalian cells. Bioluminescent imaging of parasite replication showed that all three compounds reduced the parasite burden in the murine model, with no apparent toxicity.

Original languageEnglish
Pages (from-to)3598-3601
Number of pages4
JournalAntimicrobial agents and chemotherapy
Volume59
Issue number6
DOIs
StatePublished - Jun 1 2015

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    Vasquez, M. A., Iniguez, E., Das, U., Beverley, S. M., Herrera, L. J., Dimmock, J. R., & Maldonado, R. A. (2015). Evaluation of α,β-unsaturated ketones as antileishmanial agents. Antimicrobial agents and chemotherapy, 59(6), 3598-3601. https://doi.org/10.1128/AAC.04056-14