ArticleMolecules (Basel, Switzerland)2012
New trifluoromethyl triazolopyrimidines as anti-Plasmodium falciparum agents.
Article in Molecules (Basel, Switzerland), 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
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Who cites it
11 citing papers in PubMed.
- Diverse Biological Activity of Pyrimidine Derivatives: A Review.Current drug discovery technologies · 2026Review
- Inhibition Mechanism and Target Reassessment of Potent Piperaquine Analogs: Evidence forACS omega · 2025Article
- Phenotypic screening reveals a highly selective phthalimide-based compound with antileishmanial activity.PLoS neglected tropical diseases · 2024Article
- Insights into the medicinal chemistry of heterocycles integrated with a pyrazolo[1,5-RSC medicinal chemistry · 2022Review
- Antimalarial Inhibitors Targeting Epigenetics or Mitochondria inMolecules (Basel, Switzerland) · 2021Review
- Synthesis and Bioactivity of Phthalimide Analogs as Potential Drugs to Treat Schistosomiasis, a Neglected Disease of Poverty.Pharmaceuticals (Basel, Switzerland) · 2020Article
- The Development of Novel Compounds Against Malaria: Quinolines, Triazolpyridines, Pyrazolopyridines and Pyrazolopyrimidines.Molecules (Basel, Switzerland) · 2019Review
- Synthesis, Physico-chemical Characterization, Crystal Structure and Influence on Microbial and Tumor Cells of Some Co(II) Complexes with 5,7-Dimethyl-1,2,4-triazolo[1,5-a]pyrimidine.Molecules (Basel, Switzerland) · 2017Article
- Megazol and its bioisostere 4H-1,2,4-triazole: comparing the trypanocidal, cytotoxic and genotoxic activities and their in vitro and in silico interactions with the Trypanosoma brucei nitroreductase enzyme.Memorias do Instituto Oswaldo Cruz · 2014Article
- Synthesis and isomerization of some novel pyrazolopyrimidine and pyrazolotriazolopyrimidine derivatives.Molecules (Basel, Switzerland) · 2014Article
- Anthracene-polyamine conjugates inhibit in vitro proliferation of intraerythrocytic Plasmodium falciparum parasites.Antimicrobial agents and chemotherapy · 2013Article
Corrections and comments
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Authors and funding
15 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
According to the World Health Organization, half of the World's population, approximately 3.3 billion people, is at risk for developing malaria. Nearly 700,000 deaths each year are associated with the disease. Control of the disease in humans still relies on chemotherapy. Drug resistance is a limiting factor, and the search for new drugs is important. We have designed and synthesized new 2-(trifluoromethyl)[1,2,4]triazolo[1,5-a]pyrimidine derivatives based on bioisosteric replacement of functional groups on the anti-malarial compounds mefloquine and amodiaquine. This approach enabled us to investigate the impact of: (i) ring bioisosteric replacement; (ii) a CF₃ group substituted at the 2-position of the [1,2,4]triazolo[1,5-a]pyrimidine scaffold and (iii) a range of amines as substituents at the 7-position of the of heterocyclic ring; on in vitro activity against Plasmodium falciparum. P. falciparum dihydroorotate dehydrogenase (PfDHODH) through strong hydrogen bonds. The presence of a trifluoromethyl group at the 2-position of the [1,2,4]triazolo[1,5-a]pyrimidine ring led to increased drug activity. Thirteen compounds were found to be active, with IC₅₀ values ranging from 0.023 to 20 μM in the anti-HRP2 and hypoxanthine assays. The selectivity index (SI) of the most active derivatives 5, 8, 11 and 16 was found to vary from 1,003 to 18,478.
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