“Seasoning” antimalarial drugs' action: chloroquine bile salts as novel triple-stage antiplasmodial hits

Ana Teresa Silva, Isabel Oliveira, Denise Duarte, Diana Moita, Miguel Prudêncio, Fátima Nogueira, Ricardo Ferraz, Eduardo Figueira Marques, Paula Gomes

Research output: Contribution to journalArticlepeer-review

Abstract

Malaria is one of the “big three” global infectious diseases, having caused above two hundred million cases and over half a million deaths in 2020. The continuous demand for new treatment options prioritizes the cost-effective development of new chemical entities with multi-stage antiplasmodial activity, for higher efficacy and lower propensity to elicit drug-resistant parasite strains. Following up on our long-term research towards the rescue of classical antimalarial aminoquinolines like chloroquine and primaquine, we have developed new organic salts by acid-base pairing of those drugs with natural bile acids. These antimalarial drug-derived bile salts were screened in vitro against the hepatic, blood and gametocyte stages of Plasmodium parasites, unveiling chloroquine bile salts as unprecedented triple-stage antiplasmodial hits. These findings pave a new pathway for drug rescuing, even beyond anti-malarial and other anti-infective drugs.

Original languageEnglish
JournalRSC Medicinal Chemistry
DOIs
Publication statusAccepted/In press - 2024

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