ArticleMalaria journal2018
New endoperoxides highly active in vivo and in vitro against artemisinin-resistant Plasmodium falciparum.
Article in Malaria journal, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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Who cites it
12 citing papers in PubMed.
- Synthesis, Structure, and Antileishmanial Activity of Novel 1,2,4-Trioxolanes, 1,2,4,5-Tetraoxanes and Their Respective Deoxygenated Controls.ChemMedChem · 2026Article
- Synthesis, antimalarial activity, and cytotoxicity of ethyl 4-oxocyclohexane-1-carboxylate-based 1,2,4,5-tetraoxanes: anRSC advances · 2026Article
- Design, Synthesis, and Antimalarial Evaluation of New Spiroacridine Derivatives.Antibiotics (Basel, Switzerland) · 2025Article
- A metabolite-based resistance mechanism against malaria.Science (New York, N.Y.) · 2025Article
- Enhanced Antimalarial Activity of Extracts ofChem & bio engineering · 2024Article
- Biodereplication of Antiplasmodial Extracts: Application of the Amazonian Medicinal PlantMolecules (Basel, Switzerland) · 2022Article
- Synthesis, Structure and Antileishmanial Evaluation of Endoperoxide-Pyrazole Hybrids.Molecules (Basel, Switzerland) · 2022Article
- 1,2,4-Trioxolane and 1,2,4,5-Tetraoxane Endoperoxides against Old-WorldPharmaceuticals (Basel, Switzerland) · 2022Article
- Daily rhythms of both host and parasite affect antimalarial drug efficacy.Evolution, medicine, and public health · 2021Article
- Antimalarial Agents as Therapeutic Tools Against Toxoplasmosis-A Short Bridge between Two Distant Illnesses.Molecules (Basel, Switzerland) · 2020Review
- An epigrammatic status of the 'RSC medicinal chemistry · 2020Review
- Synthesis and Antileishmanial Activity of 1,2,4,5-Tetraoxanes againstMolecules (Basel, Switzerland) · 2020Article
Corrections and comments
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Authors and funding
8 authors.
Funding
Abstract
backgroundThe emergence and spread of Plasmodium falciparum resistance to artemisinin-based combination therapy in Southeast Asia prompted the need to develop new endoperoxide-type drugs.
methodsA chemically diverse library of endoperoxides was designed and synthesized. The compounds were screened for in vitro and in vivo anti-malarial activity using, respectively, the SYBR Green I assay and a mouse model. Ring survival and mature stage survival assays were performed against artemisinin-resistant and artemisinin-sensitive P. falciparum strains. Cytotoxicity was evaluated against mammalian cell lines V79 and HepG2, using the MTT assay.
resultsThe synthesis and anti-malarial activity of 21 new endoperoxide-derived compounds is reported, where the peroxide pharmacophore is part of a trioxolane (ozonide) or a tetraoxane moiety, flanked by adamantane and a substituted cyclohexyl ring. Eight compounds exhibited sub-micromolar anti-malarial activity (IC
conclusionThe investigated, trioxolane-tetrazole conjugates LC131 and LC136 emerged as potential anti-malarial candidates; they show negligible toxicity towards mammalian cells, ability to kill intra-erythrocytic asexual stages of artemisinin-resistant P. falciparum and capacity to totally suppress P. berghei parasitaemia in mice.
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