ArticleScientific reports2023
Antiplasmodial activity, structure-activity relationship and studies on the action of novel benzimidazole derivatives.
Article in Scientific reports, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.
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Who cites it
7 citing papers in PubMed.
- PCA-mapping and machine learning identify multiple chemotypes with antiplasmodial, β-haematin and haemozoin formation inhibition activity.RSC medicinal chemistry · 2026Article
- Twenty Years of Benzimidazole Scaffold Optimization in Antiparasitic Drug Discovery.ChemMedChem · 2026Review
- Synthesis of piperazine-based benzimidazole derivatives as potent urease inhibitors and molecular docking studies.Scientific reports · 2025Article
- Benzimidazole derivatives as potentFuture medicinal chemistry · 2025Article
- Article
- Insights into the Antiparasitic Activity of Pyrazole-benzimidazole againstCurrent medicinal chemistry · 2025Article
- Design, Synthesis, Antitumor, and Antiplasmodial Evaluation of New 7-Chloroquinoline-Benzimidazole Hybrids.Molecules (Basel, Switzerland) · 2024Article
Corrections and comments
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Authors and funding
6 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Malaria cases and deaths keep being excessively high every year. Some inroads gained in the last two decades have been eroded especially due to the surge of resistance to most antimalarials. The search for new molecules that can replace the ones currently in use cannot stop. In this report, the synthesis of benzimidazole derivatives guided by structure-activity parameters is presented. Thirty-six molecules obtained are analyzed according to their activity against P. falciparum HB3 strain based on the type of substituent on rings A and B, their electron donor/withdrawing, as well as their dimension/spatial properties. There is a preference for electron donating groups on ring A, such as Me in position 5, or better, 5, 6-diMe. Ring B must be of the pyridine type such as picolinamide, other modifications are generally not favorable. Two molecules, 1 and 33 displayed antiplasmodial activity in the high nanomolar range against the chloroquine sensitive strain, with selectivity indexes above 10. Activity results of 1, 12 and 16 on a chloroquine resistance strain indicated an activity close to chloroquine for compound 1. Analysis of some of their effect on the parasites seem to suggest that 1 and 33 affect only the parasite and use a route other than interference with hemozoin biocrystallization, the route used by chloroquine and most antimalarials.
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