ArticlePloS one2012
Antimalarial activity and mechanisms of action of two novel 4-aminoquinolines against chloroquine-resistant parasites.
Article in PloS one, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
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Who cites it
18 citing papers in PubMed.
- Penicillium-Derived Inhibitors ofScientifica · 2025Article
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- Antimalarial and antioxidant activities of novel artesunate-ellagic acid hybrid compoundFrontiers in pharmacology · 2024Article
- Antiplasmodial Activity of Hydroalcoholic Extract from Jucá (Pharmaceutics · 2023Article
- In vitro and in vivo antiplasmodial activities of leaf extracts from Sonchus arvensis L.BMC complementary medicine and therapies · 2023Article
- Computational Studies of Hydroxychloroquine and Chloroquine Metabolites as Possible Candidates for Coronavirus (COVID-19) Treatment.Frontiers in pharmacology · 2020Article
- Chloroquine analogs as antimalarial candidates with potent in vitro and in vivo activity.International journal for parasitology. Drugs and drug resistance · 2018Article
- Potent Antimalarial Activity of Two Arenes Linked with Triamine Designed To Have Multiple Interactions with Heme.ACS medicinal chemistry letters · 2018Article
- Antiplasmodial activity of targeted zinc(II)-dipicolylamine complexes.Bioorganic & medicinal chemistry · 2017Article
- Anti-inflammatory activity of chloroquine and amodiaquine through p21-mediated suppression of T cell proliferation and Th1 cell differentiation.Biochemical and biophysical research communications · 2016Article
- Study of the antimalarial properties of hydroxyethylamine derivatives using green fluorescent protein transformed Plasmodium berghei.Memorias do Instituto Oswaldo Cruz · 2015Article
- Article
- In vivo antimalarial activity and mechanisms of action of 4-nerolidylcatechol derivatives.Antimicrobial agents and chemotherapy · 2015Article
- A molecular survey of febrile cases in malaria-endemic areas along China-Myanmar border in Yunnan province, People's Republic of China.Parasite (Paris, France) · 2014Article
- Antimalarial activity of 4-metoxychalcones: docking studies as falcipain/plasmepsin inhibitors, ADMET and lipophilic efficiency analysis to identify a putative oral lead candidate.Molecules (Basel, Switzerland) · 2013Article
- Aspidosperma (Apocynaceae) plant cytotoxicity and activity towards malaria parasites. Part I: Aspidosperma nitidum (Benth) used as a remedy to treat fever and malaria in the Amazon.Memorias do Instituto Oswaldo Cruz · 2013Article
- High levels of IgG3 anti ICB2-5 in Plasmodium vivax-infected individuals who did not develop symptoms.Malaria journal · 2013Article
- N-terminal Plasmodium vivax merozoite surface protein-1, a potential subunit for malaria vivax vaccine.Clinical & developmental immunology · 2013Review
Corrections and comments
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Authors and funding
8 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Chloroquine (CQ) is a cost effective antimalarial drug with a relatively good safety profile (or therapeutic index). However, CQ is no longer used alone to treat patients with Plasmodium falciparum due to the emergence and spread of CQ-resistant strains, also reported for P. vivax. Despite CQ resistance, novel drug candidates based on the structure of CQ continue to be considered, as in the present work. One CQ analog was synthesized as monoquinoline (MAQ) and compared with a previously synthesized bisquinoline (BAQ), both tested against P. falciparum in vitro and against P. berghei in mice, then evaluated in vitro for their cytotoxicity and ability to inhibit hemozoin formation. Their interactions with residues present in the NADH binding site of P falciparum lactate dehydrogenase were evaluated using docking analysis software. Both compounds were active in the nanomolar range evaluated through the HRPII and hypoxanthine tests. MAQ and BAQ derivatives were not toxic, and both compounds significantly inhibited hemozoin formation, in a dose-dependent manner. MAQ had a higher selectivity index than BAQ and both compounds were weak PfLDH inhibitors, a result previously reported also for CQ. Taken together, the two CQ analogues represent promising molecules which seem to act in a crucial point for the parasite, inhibiting hemozoin formation.
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