ArticleACS medicinal chemistry letters2013
Synthesis, Antiplasmodial Activity, and β-Hematin Inhibition of Hydroxypyridone-Chloroquine Hybrids.
Article in ACS medicinal chemistry letters, 2013. 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, 29 citations in OpenAlex.
- The Therapeutic Promise of Kojic Acid: A Comprehensive Review.Mini reviews in medicinal chemistry · 2026Review
- Hybrids/Conjugates/Chimera Drugs-Antimicrobial Hybrids: Antibiotics, Antifungals, Antituberculars, Antimalarials.Current medicinal chemistry · 2026Review
- Hybrid Molecules as Efficient Drugs against Multidrug-Resistant Malaria Parasites.ChemMedChem · 2025Review
- Quinoline as a Privileged Structure: A Recent Update on Synthesis and Biological Activities.Current topics in medicinal chemistry · 2024Review
- Synthesis, characterization, molecular docking, antimalarial, and antiproliferative activities of benzyloxy-4-oxopyridin benzoate derivatives.Research in pharmaceutical sciences · 2022Article
- Correlation between anti-malarial and anti-haemozoin activities of anti-malarial compounds.Malaria journal · 2020Article
- Deferiprone: Pan-selective Histone Lysine Demethylase Inhibition Activity and Structure Activity Relationship Study.Scientific reports · 2019Article
- Quinoline-Based Hybrid Compounds with Antimalarial Activity.Molecules (Basel, Switzerland) · 2017Review
- Insights into Integrated Lead Generation and Target Identification in Malaria and Tuberculosis Drug Discovery.Accounts of chemical research · 2017Article
- Are Antimalarial Hybrid Molecules a Close Reality or a Distant Dream?Antimicrobial agents and chemotherapy · 2017Review
- Antiplasmodial activity, in vivo pharmacokinetics and anti-malarial efficacy evaluation of hydroxypyridinone hybrids in a mouse model.Malaria journal · 2015Article
Corrections and comments
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Authors and funding
5 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
A series of noncytotoxic 4-aminoquinoline-3-hydroxypyridin-4-one hybrids were synthesized on the basis of a synergistic in vitro combination of a precursor N-alkyl-3-hydroxypyridin-4-one with chloroquine (CQ) and tested in vitro against CQ resistant (K1 and W2) and sensitive (3D7) strains of Plasmodium falciparum. In vitro antiplasmodial activity of the precursors was negated by blocking the chelator moiety via complexation with gallium(III) or benzyl protection. None of the precursors inhibited β-hematin formation. Most hybrids were more potent inhibitors of β-hematin formation than CQ, and a correlation between antiplasmodial activity and inhibition of β-hematin formation was observed. Potent hybrids against K1, 3D7, and W2, respectively, were 8c (0.13, 0.004, and 0.1 μM); 8d (0.08, 0.01, and 0.02 μM); and 7g (0.07, 0.03, and 0.08 μM).
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