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Antimicrob Agents Chemother. 2013 Jan;57(1):417-24. doi: 10.1128/AAC.00793-12. Epub 2012 Nov 5.

4(1H)-Quinolones with liver stage activity against Plasmodium berghei.

Author information

1
Department of Global Health, University of South Florida, Tampa, Florida, USA.

Abstract

With the exception of primaquine, tafenoquine, and atovaquone, there are very few antimalarials that target liver stage parasites. In this study, a transgenic Plasmodium berghei parasite (1052Cl1; PbGFP-Luc(con)) that expresses luciferase was used to assess the anti-liver stage parasite activity of ICI 56,780, a 7-(2-phenoxyethoxy)-4(1H)-quinolone (PEQ), as well as two 3-phenyl-4(1H)-quinolones (P4Q), P4Q-146 and P4Q-158, by using bioluminescent imaging (BLI). Results showed that all of the compounds were active against liver stage parasites; however, ICI 56,780 and P4Q-158 were the most active, with low nanomolar activity in vitro and causal prophylactic activity in vivo. This potent activity makes these compounds ideal candidates for advancement as novel antimalarials.

PMID:
23129047
PMCID:
PMC3535941
DOI:
10.1128/AAC.00793-12
[Indexed for MEDLINE]
Free PMC Article

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