ArticleAntimicrobial agents and chemotherapy2006
Targeting of hematin by the antimalarial pyronaridine.
Article in Antimicrobial agents and chemotherapy, 2006. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 33 papers, 1 of them a synthesis that pooled it.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
33 citing papers in PubMed, 1 synthesis or guideline pooled it, 92 citations in OpenAlex.
- Artesunate plus pyronaridine for treating uncomplicated Plasmodium falciparum malaria.The Cochrane database of systematic reviews · 2014Pooled it
- Stage-specific pharmacodynamic chloroquine and pyronaridine action on artemisinin ring-stage resistant Kelch C580Y mutationAntimicrobial agents and chemotherapy · 2025Article
- Exploring bioactive molecules released during inter- and intraspecific competition: A paradigm for novel antiparasitic drug discovery and design for human use.Current research in parasitology & vector-borne diseases · 2025Review
- Antimicrobial Activity of Naphthyridine Derivatives.Pharmaceuticals (Basel, Switzerland) · 2024Review
- Oral Pyronaridine Tetraphosphate Reduces Tissue Presence of Parasites in a Mouse Model of Chagas Disease.ACS omega · 2024Article
- Pyronaridine: a review of its clinical pharmacology in the treatment of malaria.The Journal of antimicrobial chemotherapy · 2023Review
- Novel Transmission-Blocking Antimalarials Identified by High-Throughput Screening of Plasmodium berghei Ookluc.Antimicrobial agents and chemotherapy · 2023Article
- Similarly efficacious anti-malarial drugs SJ733 and pyronaridine differ in their ability to remove circulating parasites in mice.Malaria journal · 2022Article
- Protecting future antimalarials from the trap of resistance: Lessons from artemisinin-based combination therapy (ACT) failures.Journal of pharmaceutical analysis · 2021Review
- Article
- Evidence for in vitro and in vivo activity of the antimalarial pyronaridine against Schistosoma.PLoS neglected tropical diseases · 2021Article
- Fused 1,5-Naphthyridines: Synthetic Tools and Applications.Molecules (Basel, Switzerland) · 2020Review
- Preclinical Antimalarial Combination Study of M5717, a Plasmodium falciparum Elongation Factor 2 Inhibitor, and Pyronaridine, a Hemozoin Formation Inhibitor.Antimicrobial agents and chemotherapy · 2020Article
- Resistance to Artemisinin Combination Therapies (ACTs): Do Not Forget the Partner Drug!Tropical medicine and infectious disease · 2019Review
- Identification of Anti-Trypanosoma cruzi Lead Compounds with Putative Immunomodulatory Activity.Antimicrobial agents and chemotherapy · 2018Article
- Design, synthesis and bioactivities of phenithionate analogues or derivatives for anti-schistosomiasis.MedChemComm · 2018Article
- Pyronaridine exerts potent cytotoxicity on human breast and hematological cancer cells through induction of apoptosis.PloS one · 2018Article
- Novel carbazole aminoalcohols as inhibitors of β-hematin formation: Antiplasmodial and antischistosomal activities.International journal for parasitology. Drugs and drug resistance · 2017Article
- Anti-plasmodial and Chloroquine Resistance Suppressive Effects of Embelin.Pharmacognosy magazine · 2017Article
- Review
Corrections and comments
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Authors and funding
5 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Pyronaridine, 2-methoxy-7-chloro-10[3',5'-bis(pyrrolidinyl-1-methyl-)4'hydroxyphenyl]aminobenzyl-(b)-1,5-naphthyridine, a new Mannich base schizontocide originally developed in China and structurally related to the aminoacridine drug quinacrine, is currently undergoing clinical testing. We now show that pyronaridine targets hematin, as demonstrated by its ability to inhibit in vitro beta-hematin formation (at a concentration equal to that of chloroquine), to form a complex with hematin with a stoichiometry of 1:2, to enhance hematin-induced red blood cell lysis (but at 1/100 of the chloroquine concentration), and to inhibit glutathione-dependent degradation of hematin. Our observations that pyronaridine exerted this mechanism of action in situ, based on growth studies of Plasmodium falciparum K1 in culture showing antagonism of pyronaridine in combination with antimalarials (chloroquine, mefloquine, and quinine) that inhibit beta-hematin formation, were equivocal.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.