ArticleAntimicrobial agents and chemotherapy2016
Targeting the Cytochrome bc1 Complex of Leishmania Parasites for Discovery of Novel Drugs.
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 32 papers.
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Who cites it
32 citing papers in PubMed, 43 citations in OpenAlex.
- Potential efficacy of repurposed drugs for treating drug-resistant visceral leishmaniasis.Naunyn-Schmiedeberg's archives of pharmacology · 2026Article
- ExploringAntimicrobial agents and chemotherapy · 2026Article
- Heme limitation induces LHR2, an essential gene for Leishmania pathogenesis.PLoS pathogens · 2026Article
- Untargeted metabolomics for triaging of cytochrome b inhibitors during Chagas' disease drug discovery.PLoS neglected tropical diseases · 2026Article
- Article
- Plant-derived products as anti-leishmanials which target mitochondria: a review.Expert reviews in molecular medicine · 2025Review
- Pharmacological inhibition of key metabolic pathways attenuates Leishmania spp infection in macrophages.PLoS neglected tropical diseases · 2025Article
- Oxidative Stress and Erectile Dysfunction: Pathophysiology, Impacts, and Potential Treatments.Current issues in molecular biology · 2024Review
- Discovery and Optimization of Tambjamines as a Novel Class of Antileishmanial Agents.Journal of medicinal chemistry · 2024Article
- Synthesis of Deuterated Endochin-Like Quinolones.Journal of labelled compounds & radiopharmaceuticals · 2024Article
- 4-Aminoquinoline as a privileged scaffold for the design of leishmanicidal agents: structure-property relationships and key biological targets.Frontiers in chemistry · 2024Review
- Drug Discovery for Cutaneous Leishmaniasis: A Review of Developments in the Past 15 Years.Microorganisms · 2023Review
- Quinolone-3-amidoalkanol: A New Class of Potent and Broad-Spectrum Antimicrobial Agent.ACS omega · 2023Article
- The critical role of mode of action studies in kinetoplastid drug discovery.Frontiers in drug discovery · 2023Article
- In Vitro versus in Mice: Efficacy and Safety of Decoquinate and Quinoline-Pathogens (Basel, Switzerland) · 2023Article
- Systems biology of autophagy in leishmanial infection and its diverse role in precision medicine.Frontiers in molecular biosciences · 2023Review
- Naphthoquinone as a New Chemical Scaffold for Leishmanicidal Inhibitors ofBiomedicines · 2022Article
- Treatment of Human Babesiosis: Then and Now.Pathogens (Basel, Switzerland) · 2021Review
- Amino-Substituted 3-Aryl- and 3-Heteroarylquinolines as Potential Antileishmanial Agents.Journal of medicinal chemistry · 2021Article
- In Silico Insights into the Mechanism of Action of Epoxy-α-Lapachone and Epoxymethyl-Lawsone inMolecules (Basel, Switzerland) · 2021Article
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Authors and funding
11 authors at 2 institutions in 1 country.
Funding
Abstract
Endochin-like quinolones (ELQs) are potent and specific inhibitors of cytochrome bc1 from Plasmodium falciparum and Toxoplasma gondii and show promise for novel antiparasitic drug development. To determine whether the mitochondrial electron transport chain of Leishmania parasites could be targeted similarly for drug development, we investigated the activity of 134 structurally diverse ELQs. A cohort of ELQs was selectively toxic to amastigotes of Leishmania mexicana and L. donovani, with 50% inhibitory concentrations (IC50s) in the low micromolar range, but the structurally similar hydroxynaphthoquinone buparvaquone was by far the most potent inhibitor of electron transport, ATP production, and intracellular amastigote growth. Cytochrome bc1 is thus a promising target for novel antileishmanial drugs, and further improvements on the buparvaquone scaffold are warranted for development of enhanced therapeutics.
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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.