Abstract
Previous studies have reported the use of nitrogen-heterocyclic compounds to treat malaria. Interestingly, quinolone and 1,2,4-triazole scaffolds demonstrated an outstanding capacity to target at least two stages of the malaria parasite life cycle, especially when they are hybrid with other nitrogen heterocycles. Thus, the objective of this study is to assess the drug susceptibility of Plasmodium knowlesi A1H1 parasites to certain 1,2,4-triazoles and benzoquinones that bear pyrrolidinones using a plasmodium lactate dehydrogenase assay. All synthesized compounds showed moderate activity against P. knowlesi A1H1 with EC50 values in the range of 13.39-28.85 μM. Both 1,2,4-triazoles and quinolone derivatives were synthesized using commercially available pyrrolidinones.
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