ArticleAntimicrobial agents and chemotherapy2013
Defining the timing of action of antimalarial drugs against Plasmodium falciparum.
Article in Antimicrobial agents and chemotherapy, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 71 papers.
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71 citing papers in PubMed, 185 citations in OpenAlex.
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- Unpacking boxes: identification of novel inhibitors of malaria parasite invasion.International journal for parasitology. Drugs and drug resistance · 2026Article
- Ruthenium Complexes of Atovaquone Acting on Multiple Stages of theJournal of medicinal chemistry · 2026Article
- Identification of α-Azacyclic Acetamide-Based Inhibitors ofACS infectious diseases · 2025Article
- Detection of novelMicrobial genomics · 2025Article
- Antimalarial and neuroprotective effects of ethanolic extracts of the five-flower remedy in an experimental cerebral malaria model.PloS one · 2025Article
- Integral Solvent-Induced Protein Precipitation for Target-Engagement Studies inACS infectious diseases · 2024Article
- Real-time measurements of ATP dynamics via ATeams inAntimicrobial agents and chemotherapy · 2024Article
- Enhanced Antimalarial and Antisequestration Activity of Methoxybenzenesulfonate-Modified Biopolymers and Nanoparticles for Tackling Severe Malaria.ACS infectious diseases · 2024Article
- Efficacy of artesunate combined with Atractylodes lancea or Prabchompoothaweep remedy extracts as adjunctive therapy for the treatment of cerebral malaria.BMC complementary medicine and therapies · 2023Article
- Sulfonylpiperazine compounds prevent Plasmodium falciparum invasion of red blood cells through interference with actin-1/profilin dynamics.PLoS biology · 2023Article
- Cripowellins PauseMolecules (Basel, Switzerland) · 2023Article
- Antimalarial effect of synthetic endoperoxide on synchronized Plasmodium chabaudi infected mice.Parasites, hosts and diseases · 2023Article
- Promising Antiparasitic Natural and Synthetic Products from Marine Invertebrates and Microorganisms.Marine drugs · 2023Review
- Erythrocyte membrane with CLIPPKF as biomimetic nanodecoy traps merozoites and attaches to infected red blood cells to prevent Plasmodium infection.Journal of nanobiotechnology · 2023Article
- High-throughput analysis of the transcriptional patterns of sexual genes in malaria.Parasites & vectors · 2023Article
- In Vitro Evaluation of Two Novel Antimalarial Derivatives of SKM13: SKM13-MeO and SKM13-F.The Korean journal of parasitology · 2022Article
- Parasite Viability as a Measure ofAntimicrobial agents and chemotherapy · 2022Article
- Optimizing bulk segregant analysis of drug resistance usingiScience · 2022Article
11 more citing papers are in PubMed but not listed here.
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Authors and funding
5 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Most current antimalarials for treatment of clinical Plasmodium falciparum malaria fall into two broad drug families and target the food vacuole of the trophozoite stage. No antimalarials have been shown to target the brief extracellular merozoite form of blood-stage malaria. We studied a panel of 12 drugs, 10 of which have been used extensively clinically, for their invasion, schizont rupture, and growth-inhibitory activity using high-throughput flow cytometry and new approaches for the study of merozoite invasion and early intraerythrocytic development. Not surprisingly, given reported mechanisms of action, none of the drugs inhibited merozoite invasion in vitro. Pretreatment of erythrocytes with drugs suggested that halofantrine, lumefantrine, piperaquine, amodiaquine, and mefloquine diffuse into and remain within the erythrocyte and inhibit downstream growth of parasites. Studying the inhibitory activity of the drugs on intraerythrocytic development, schizont rupture, and reinvasion enabled several different inhibitory phenotypes to be defined. All drugs inhibited parasite replication when added at ring stages, but only artesunate, artemisinin, cycloheximide, and trichostatin A appeared to have substantial activity against ring stages, whereas the other drugs acted later during intraerythrocytic development. When drugs were added to late schizonts, only artemisinin, cycloheximide, and trichostatin A were able to inhibit rupture and subsequent replication. Flow cytometry proved valuable for in vitro assays of antimalarial activity, with the free merozoite population acting as a clear marker for parasite growth inhibition. These studies have important implications for further understanding the mechanisms of action of antimalarials, studying and evaluating drug resistance, and developing new antimalarials.
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