ArticleACS medicinal chemistry letters2014
Novel endoperoxide-based transmission-blocking antimalarials with liver- and blood-schizontocidal activities.
Article in ACS medicinal chemistry letters, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
What it found
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The trial behind it
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
16 citing papers in PubMed.
- Hybrids/Conjugates/Chimera Drugs-Antimicrobial Hybrids: Antibiotics, Antifungals, Antituberculars, Antimalarials.Current medicinal chemistry · 2026Review
- Updates on traditional methods for combating malaria and emergingFrontiers in cellular and infection microbiology · 2024Review
- Putative Contribution of 8-Aminoquinolines to Preventing Recrudescence of Malaria.Tropical medicine and infectious disease · 2023Article
- A Hybrid of Amodiaquine and Primaquine Linked by Gold(I) Is a Multistage Antimalarial Agent Targeting Heme Detoxification and Thiol Redox Homeostasis.Pharmaceutics · 2022Article
- Transmission-Blocking Strategies Against Malaria Parasites During Their Mosquito Stages.Frontiers in cellular and infection microbiology · 2022Review
- 5-Phenoxy Primaquine Analogs and the Tetraoxane Hybrid as Antimalarial Agents.Molecules (Basel, Switzerland) · 2021Article
- Synthesis of Novel Ciprofloxacin-Based Hybrid Molecules toward Potent Antimalarial Activity.ACS medicinal chemistry letters · 2020Article
- An Overview of Drug Resistance in Protozoal Diseases.International journal of molecular sciences · 2019Review
- Primaquine derivatives: Modifications of the terminal amino group.European journal of medicinal chemistry · 2019Review
- Primaquine-quinoxaline 1,4-di-N-oxide hybrids with action on the exo-erythrocytic forms of Plasmodium induce their effect by the production of reactive oxygen species.Malaria journal · 2019Article
- Synthesis of Thymoquinone-Artemisinin Hybrids: New Potent Antileukemia, Antiviral, and Antimalarial Agents.ACS medicinal chemistry letters · 2018Article
- Quinoline-Based Hybrid Compounds with Antimalarial Activity.Molecules (Basel, Switzerland) · 2017Review
- Synthesis of Novel Hybrids of Quinazoline and Artemisinin with High Activities againstACS omega · 2017Article
- Are Antimalarial Hybrid Molecules a Close Reality or a Distant Dream?Antimicrobial agents and chemotherapy · 2017Review
- Antimalarial and antimicrobial activities of 8-Aminoquinoline-Uracils metal complexes.EXCLI journal · 2016Article
- Antimalarial chemotherapy: orally curative artemisinin-derived trioxane dimer esters.Bioorganic & medicinal chemistry letters · 2015Article
Corrections and comments
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Authors and funding
16 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
In a search for effective compounds against both the blood- and liver-stages of infection by malaria parasites with the ability to block the transmission of the disease to mosquito vectors, a series of hybrid compounds combining either a 1,2,4-trioxane or 1,2,4,5-tetraoxane and 8-aminoquinoline moieties were synthesized and screened for their antimalarial activity. These hybrid compounds showed high potency against both exoerythrocytic and erythrocytic forms of malaria parasites, comparable to representative trioxane-based counterparts. Furthermore, they efficiently blocked the development of the sporogonic cycle in the mosquito vector. The tetraoxane-based hybrid 5, containing an amide linker between the two moieties, effectively cleared a patent blood-stage P. berghei infection in mice after i.p. administration. Overall, these results indicate that peroxide-8-aminoquinoline hybrids are excellent starting points to develop an agent that conveys all the desired antimalarial multistage activities in a single chemical entity and, as such, with the potential to be used in malaria elimination campaigns.
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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.