Autor(es): Fonte, Mélanie ; Tassi, Natália ; Fontinha, Diana ; Bóuzon-Arnáiz, Inês ; Ferraz, Ricardo ; Araújo, Maria J. ; Fèrnandez-Busquets, Xavier ; Prudêncio, Miguel ; Gomes, Paula ; Teixeira, Cátia
Data: 2020
Identificador Persistente: http://hdl.handle.net/10400.22/16648
Origem: Repositório Científico do Instituto Politécnico do Porto
Assunto(s): 4,9‐Diaminoacridines; 4‐Aminoacridines; Antiplasmodial
Multi‐stage drugs have been prioritized in antimalarial drug discovery, as targeting more than one process in the Plasmodium life cycle is likely to increase efficiency, while decreasing the chances of emergence of resistance by the parasite. Herein, we disclose two novel acridine‐based families of compounds that combine the structural features of primaquine and chloroquine. Compounds prepared and studied thus far retained the in vitro activity displayed by the parent drugs against the erythrocytic stages of chloroquine‐sensitive and ‐resistant Plasmodium falciparum strains, and against the hepatic stages of Plasmodium berghei, hence acting as dual‐stage antiplasmodial hits.
