ArticlePloS one2014
Evaluation of antimalarial activity and toxicity of a new primaquine prodrug.
Article in PloS one, 2014. 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, 51 citations in OpenAlex.
- Synthesis, characterization, and biological activities of two new pyrazole Schiff base derivatives.Scientific reports · 2026Article
- Lactobionic Acid as a Biocompatibility Switch: Physicochemical and Biological Characterization of Copper(II)-Primaquine Complexes.Bioinorganic chemistry and applications · 2026Article
- Novel heterospirocyclic antimalarials with activity against artemisinin- and multidrug-resistant P. falciparum malaria.International journal for parasitology. Drugs and drug resistance · 2025Article
- In vitro and in vivo antiplasmodial activities of leaf extracts from Sonchus arvensis L.BMC complementary medicine and therapies · 2023Article
- Article
- Primaquine derivatives: Modifications of the terminal amino group.European journal of medicinal chemistry · 2019Review
- 8-Aminoquinoline Therapy for Latent Malaria.Clinical microbiology reviews · 2019Review
- In vitro antiplasmodial activity, pharmacokinetic profiles and interference in isoprenoid pathway of 2-aniline-3-hydroxy-1.4-naphthoquinone derivatives.Malaria journal · 2018Article
- Cytotoxicity, hemolysis andToxicology reports · 2016Article
- Chloroquine analogues in drug discovery: new directions of uses, mechanisms of actions and toxic manifestations from malaria to multifarious diseases.The Journal of antimicrobial chemotherapy · 2015Review
- Side Effects of Chloroquine and Primaquine and Symptom Reduction in Malaria Endemic Area (Mâncio Lima, Acre, Brazil).Interdisciplinary perspectives on infectious diseases · 2015Article
Corrections and comments
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Authors and funding
11 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Plasmodium vivax is the most prevalent of the five species causing malaria in humans. The current available treatment for P. vivax malaria is limited and unsatisfactory due to at least two drawbacks: the undesirable side effects of primaquine (PQ) and drug resistance to chloroquine. Phenylalanine-alanine-PQ (Phe-Ala-PQ) is a PQ prodrug with a more favorable pharmacokinetic profile compared to PQ. The toxicity of this prodrug was evaluated in in vitro assays using a human hepatoma cell line (HepG2), a monkey kidney cell line (BGM), and human red blood cells deficient in the enzyme glucose-6-phosphate-dehydrogenase (G6PD). In addition, in vivo toxicity assays were performed with rats that received multiple doses of Phe-Ala-PQ to evaluate biochemical, hematological, and histopathological parameters. The activity was assessed by the inhibition of the sporogonic cycle using a chicken malaria parasite. Phe-Ala-PQ blocked malaria transmission in Aedes mosquitoes. When compared with PQ, it was less cytotoxic to BGM and HepG2 cells and caused less hemolysis of G6PD-deficient red blood cells at similar concentrations. The prodrug caused less alteration in the biochemical parameters than did PQ. Histopathological analysis of the liver and kidney did show differences between the control and Phe-Ala-PQ-treated groups, but they were not statistically significant. Taken together, the results highlight the prodrug as a novel lead compound candidate for the treatment of P. vivax malaria and as a blocker of malaria transmission.
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