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

• Tipo: Artigo em Revista Científica Internacional
• Data: 2024

Autores

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

Revista

Título: RSC Medicinal Chemistry

Editora: Royal Society of Chemistry

Indexação

ISI Web of Knowledge - 1 Citação

Scopus - 1 Citação

Outras Informações

ID Authenticus: 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.

Idioma: Inglês

Tipo (Avaliação Docente): Científica

Nº de páginas: 6