ArticleMolecular and biochemical parasitology2011
Design of anti-parasitic and anti-fungal hydroxy-naphthoquinones that are less susceptible to drug resistance.
Article in Molecular and biochemical parasitology, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Who cites it
17 citing papers in PubMed, 56 citations in OpenAlex.
- Pharmacomodulation of the Redox-Active Lead Plasmodione: Synthesis of Substituted 2-Benzylnaphthoquinone Derivatives, Antiplasmodial Activities, and Physicochemical Properties.International journal of molecular sciences · 2025Article
- Fabrication of Phytosome with Enhanced Activity ofInternational journal of nanomedicine · 2024Article
- The Relevance and Insights on 1,4-Naphthoquinones as Antimicrobial and Antitumoral Molecules: A Systematic Review.Pharmaceuticals (Basel, Switzerland) · 2023Review
- In Vitro Antimicrobial Effects and Inactivation Mechanisms of 5,8-Dihydroxy-1,4-Napthoquinone.Antibiotics (Basel, Switzerland) · 2022Article
- 2-hydroxy-1,4-naphthoquinones with 3-alkyldiarylether groups: synthesis andFuture medicinal chemistry · 2022Article
- Efficient Oxidative Dearomatisations of Substituted Phenols Using Hypervalent Iodine (III) Reagents and Antiprotozoal Evaluation of the Resulting Cyclohexadienones againstMolecules (Basel, Switzerland) · 2022Article
- Catalytic Reactions and Energy Conservation in the CytochromeChemical reviews · 2021Review
- Prenylquinones in Human Parasitic Protozoa: Biosynthesis, Physiological Functions, and Potential as Chemotherapeutic Targets.Molecules (Basel, Switzerland) · 2019Review
- Curcumin nanoemulsion as a novel chemical for the treatment of acute and chronic toxoplasmosis in mice.International journal of nanomedicine · 2018Article
- Electronic connection between the quinone and cytochrome C redox pools and its role in regulation of mitochondrial electron transport and redox signaling.Physiological reviews · 2015Article
- Biological evaluation of hydroxynaphthoquinones as anti-malarials.Malaria journal · 2013Article
- Synergism of antifungal activity between mitochondrial respiration inhibitors and kojic acid.Molecules (Basel, Switzerland) · 2013Article
- Reconstructing the Qo site of Plasmodium falciparum bc 1 complex in the yeast enzyme.PloS one · 2013Article
- Significant reduction of brain cysts caused by Toxoplasma gondii after treatment with spiramycin coadministered with metronidazole in a mouse model of chronic toxoplasmosis.Antimicrobial agents and chemotherapy · 2012Article
- Cytochrome b mutation Y268S conferring atovaquone resistance phenotype in malaria parasite results in reduced parasite bc1 catalytic turnover and protein expression.The Journal of biological chemistry · 2012Article
- Mitochondria and trypanosomatids: targets and drugs.Pharmaceutical research · 2011Review
- Biological Evaluation of Two 1,4-Naphthoquinone Derivatives Against a Breast Human Adenocarcinoma Cell Line.Current health sciences journalArticle
Corrections and comments
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Authors and funding
6 authors at 2 institutions in 1 country.
Funding
Abstract
Atovaquone is a hydroxy-naphthoquinone that is used to treat parasitic and fungal infections including Plasmodium falciparum (malaria), Pneumocystis jivorecii (pneumonia) and Toxoplasma gondii (toxoplasmosis). It blocks mitochondrial oxidation of ubiquinol in these organisms by binding to the ubiquinol oxidation site of the cytochrome bc(1) complex. Failure of atovaquone treatment has been linked to the appearance of mutations in the mitochondrially encoded gene for cytochrome b. In order to determine the optimal parameters required for inhibition of respiration in parasites and pathogenic fungi and overcome drug resistance, we have synthesized and tested the inhibitory activity of novel hydroxy-naphthoquinones against blood stage P. falciparum and liver stage P. berghei and against cytochrome bc(1) complexes isolated from yeast strains bearing mutations in cytochrome b associated with resistance in Plasmodium, Pneumocystis, and Toxoplasma. One of the new inhibitors is highly effective against an atovaquone resistant Plasmodium and illustrates the type of modification to the hydroxy-naphthoquinone ring of atovaquone that might mitigate drug resistance.
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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.