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

• Type: Article in International Scientific Journal
• Date: 2024

Authors

Silva, AT (Author) Other; Oliveira, I (Author) Other; Duarte, D (Author) Other; Moita, D (Author) Other; Prudencio, M (Author) Other; Nogueira, F (Author) Other; Ferraz, R (Author) Other; Eduardo F Marques (Author) FCUP; Paula Gomes (Author) FCUP

Journal

Title: RSC Medicinal Chemistry

Publisher: Royal Society of Chemistry

Indexing

ISI Web of Knowledge - 1 Citation

Scopus - 1 Citation

Other information

Authenticus ID: P-010-FYC

DOI: 10.1039/d4md00007b

Abstract (EN): 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. Malaria is one of the big three global infectious diseases, with the heaviest toll on human lives in low-to-middle income countries. Cost-effective antimalarial drugs with multi-stage action remain an unmet and urgent need in global healthcare.

Language: English

Type (Professor's evaluation): Scientific

No. of pages: 6