Document details

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

Author(s): Silva, Ana Teresa ; Oliveira, Isabel S. ; Gomes, Joana ; Aguiar, Luísa ; Fontinha, Diana ; Duarte, Denise ; Nogueira, Fátima ; Prudêncio, Miguel ; Marques, Eduardo F. ; Teixeira, Cátia ; Ferraz, Ricardo ; Gomes, Paula

Date: 2021

Persistent ID: http://hdl.handle.net/10451/51680

Origin: Repositório da Universidade de Lisboa

Project/scholarship: info:eu-repo/grantAgreement/FCT/6817 - DCRRNI ID/UIDB%2F50006%2F2020/PT; info:eu-repo/grantAgreement/FCT/6817 - DCRRNI ID/UIDB%2F00081%2F2020/PT; info:eu-repo/grantAgreement/FCT/5876/UID%2FMulti%2F04413%2F2013/PT; info:eu-repo/grantAgreement/FCT/3599-PPCDT/PTDC%2FBTM-SAL%2F29786%2F2017/PT; info:eu-repo/grantAgreement/FCT/POR_NORTE/SFRH%2FBD%2F150649%2F2020/PT;

Subject(s): Antimalarial; Plasmodium; SAIL; Blood-stage; Fatty acid; Ionic liquid; Liver-stage; Surface activity


Description

© 2021 Wiley-VCH GmbH

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.

The authors thank Fundação para a Ciência e Tecnologia (FCT, Portugal), for funding Research Units LAQV-REQUIMTE (UIDB/50006/2020), CIQUP (UIDB/00081/2020), and GHTM (UID/Multi/04413/2013), and for project grant PTDC/BTM-SAL/29786/2017. ATS thanks FCT and Sociedade Portuguesa de Química (SPQ, Portugal) for her doctoral grant SFRH/BD/150649/2020

Document Type Journal article
Language English
Contributor(s) Repositório da Universidade de Lisboa
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