ArticleJournal of medicinal chemistry2009
Imidazoquines as antimalarial and antipneumocystis agents.
Article in Journal of medicinal chemistry, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 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
12 citing papers in PubMed.
- Repositioning Brusatol as a Transmission Blocker of Malaria Parasites.ACS infectious diseases · 2024Article
- "Seasoning" antimalarial drugs' action: chloroquine bile salts as novel triple-stage antiplasmodial hits.RSC medicinal chemistry · 2024Article
- Reaction of Picolinamides with Ketones Producing a New Type of Heterocyclic Salts with an Imidazolidin-4-One Ring.Molecules (Basel, Switzerland) · 2023Article
- The monoterpene 1,8-cineole prevents cerebral edema in a murine model of severe malaria.PloS one · 2022Article
- Coupling the Antimalarial Cell Penetrating Peptide TP10 to Classical Antimalarial Drugs Primaquine and Chloroquine Produces Strongly Hemolytic Conjugates.Molecules (Basel, Switzerland) · 2019Article
- Primaquine derivatives: Modifications of the terminal amino group.European journal of medicinal chemistry · 2019Review
- Coupling the cell-penetrating peptides transportan and transportan 10 to primaquine enhances its activity against liver-stage malaria parasites.MedChemComm · 2019Article
- Chloroquine Analogues as Leads against Pneumocystis Lung Pathogens.Antimicrobial agents and chemotherapy · 2018Article
- Synthesis of Polycyclic Imidazolidinones via Amine Redox-Annulation.Organic letters · 2017Article
- Article
- Peptidomimetic and organometallic derivatives of primaquine active against Leishmania infantum.Antimicrobial agents and chemotherapy · 2012Article
- Novel potent metallocenes against liver stage malaria.Antimicrobial agents and chemotherapy · 2012Article
Corrections and comments
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Authors and funding
13 authors.
Funding
Abstract
Peptidomimetic imidazolidin-4-one derivatives of primaquine (imidazoquines) recently displayed in vitro activity against blood schizonts of a chloroquine-resistant strain of Plasmodium falciparum. Preliminary studies with a subset of such imidazoquines showed them to both block transmission of P. berghei malaria from mouse to mosquito and be highly stable toward hydrolysis at physiological conditions. This prompted us to have deeper insight into the activity of imidazoquines against both Plasmodia and Pneumocystis carinii, on which primaquine is also active. Full assessment of the in vivo transmission-blocking activity of imidazoquines, in vitro tissue-schizontocidal activity on P. berghei-infected hepatocytes, and in vitro anti-P. carinii activity is now reported. All compounds were active in these biological assays, with generally lower activity than the parent drug. However, imidazoquines' stability against both oxidative deamination and proteolytic degradation suggest that they will probably have higher oral bioavailability and lower hematotoxicity than primaquine, which might translate into higher therapeutic indexes.
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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.