ArticleAntimicrobial agents and chemotherapy2016
The Redox Cycler Plasmodione Is a Fast-Acting Antimalarial Lead Compound with Pronounced Activity against Sexual and Early Asexual Blood-Stage Parasites.
Article in Antimicrobial agents and chemotherapy, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
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Who cites it
18 citing papers in PubMed.
- Ruthenium Complexes of Atovaquone Acting on Multiple Stages of theJournal of medicinal chemistry · 2026Article
- The heme A synthase Cox15, as a target of redox-active 3-benzylmenadiones with antiparasitic activity.Antimicrobial agents and chemotherapy · 2026Article
- Synthesis, Antiprotozoal Activity, and Physicochemical Evaluation of Benzamido-Menadione Derivatives.International journal of molecular sciences · 2025Article
- Marine Guanidine Alkaloids Inhibit Malaria Parasites Development inACS infectious diseases · 2025Article
- Design, Synthesis and Antiplasmodial Activities of a Library of Fluorine-Based 3-Benzylmenadiones.Molecules (Basel, Switzerland) · 2025Article
- Synthesis of 1,2,3-Triazole-Methyl-Menadione Derivatives: Evaluation of Electrochemical and Antiparasitic Properties against two Blood-Dwelling Parasites.ChemMedChem · 2025Article
- Pharmacomodulation of the Redox-Active Lead Plasmodione: Synthesis of Substituted 2-Benzylnaphthoquinone Derivatives, Antiplasmodial Activities, and Physicochemical Properties.International journal of molecular sciences · 2025Article
- Uncovering the Mechanism of Action of Antiprotozoal Agents: A Survey on Photoaffinity Labeling Strategy.Pharmaceuticals (Basel, Switzerland) · 2024Review
- Regioselective Synthesis of Potential Non-Quinonoid Prodrugs of Plasmodione: Antiparasitic Properties Against Two Hemoglobin-Feeding Parasites and Drug Metabolism Studies.Molecules (Basel, Switzerland) · 2024Article
- Metal(triphenylphosphine)-atovaquone Complexes: Synthesis, Antimalarial Activity, and Suppression of Heme Detoxification.Inorganic chemistry · 2024Article
- Real-time measurements of ATP dynamics via ATeams inAntimicrobial agents and chemotherapy · 2024Article
- Aptamer-based nanotrains and nanoflowers as quinine delivery systems.International journal of pharmaceutics: X · 2023Article
- Antimalarial and antitumour activities of the steroidal quinone-methide celastrol and its combinations with artemiside, artemisone and methylene blue.Frontiers in pharmacology · 2022Article
- The evaluation of ADME and pharmacokinetic properties of decoquinate derivatives for the treatment of malaria.Frontiers in pharmacology · 2022Article
- Menadione: a platform and a target to valuable compounds synthesis.Beilstein journal of organic chemistry · 2022Review
- Syk Kinase Inhibitors Synergize with Artemisinins by Enhancing Oxidative Stress inAntioxidants (Basel, Switzerland) · 2020Article
- AntimalarialACS medicinal chemistry letters · 2020Article
- Pharmacomodulation of the Antimalarial Plasmodione: Synthesis of Biaryl- and N-Arylalkylamine Analogues, Antimalarial Activities and Physicochemical Properties.Molecules (Basel, Switzerland) · 2017Article
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12 authors.
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Abstract
Previously, we presented the chemical design of a promising series of antimalarial agents, 3-[substituted-benzyl]-menadiones, with potent in vitro and in vivo activities. Ongoing studies on the mode of action of antimalarial 3-[substituted-benzyl]-menadiones revealed that these agents disturb the redox balance of the parasitized erythrocyte by acting as redox cyclers-a strategy that is broadly recognized for the development of new antimalarial agents. Here we report a detailed parasitological characterization of the in vitro activity profile of the lead compound 3-[4-(trifluoromethyl)benzyl]-menadione 1c (henceforth called plasmodione) against intraerythrocytic stages of the human malaria parasite Plasmodium falciparum We show that plasmodione acts rapidly against asexual blood stages, thereby disrupting the clinically relevant intraerythrocytic life cycle of the parasite, and furthermore has potent activity against early gametocytes. The lead's antiplasmodial activity was unaffected by the most common mechanisms of resistance to clinically used antimalarials. Moreover, plasmodione has a low potential to induce drug resistance and a high killing speed, as observed by culturing parasites under continuous drug pressure. Drug interactions with licensed antimalarial drugs were also established using the fixed-ratio isobologram method. Initial toxicological profiling suggests that plasmodione is a safe agent for possible human use. Our studies identify plasmodione as a promising antimalarial lead compound and strongly support the future development of redox-active benzylmenadiones as antimalarial agents.
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