Drug-derived surface-active ionic liquids: a cost-effective way to expressively increase the blood-stage antimalarial activity of primaquine

Inspired by previous disclosure of room-temperature ionic liquids derived from primaquine and cinnamic acids, which displayed slightly enhanced blood-stage activity compared to the parent drug, we have now combined this emblematic antimalarial with natural fatty acids. This affords surface-active ionic liquids whose liver-stage antiplasmodial activity is either retained or slightly enhanced, while revealing blood-stage antiplasmodial activity at least one order of magnitude higher than that of the parent compound. These findings open new perspectives towards the cost-effective recycling of classical drugs that are either shelved or in decline, and which is not limited to antimalarial agents.

Keywords

Antimalarial Blood-stage Fatty acid Ionic liquid Liver-stage Plasmodium SAIL Surface activity

URI

http://hdl.handle.net/10400.22/20410

Citation

Silva, A. T., Oliveira, I. S., Gomes, J., Aguiar, L., Fontinha, D., Duarte, D., Nogueira, F., Prudêncio, M., Marques, E. F., Teixeira, C., Ferraz, R., & Gomes, P. (2021). Drug-Derived Surface-Active Ionic Liquids: A Cost-Effective Way To Expressively Increase the Blood-Stage Antimalarial Activity of Primaquine. ChemMedChem, 17(5), e202100650. https://doi.org/https://doi.org/10.1002/cmdc.202100650