by Keyword: liver-stage
Fonte M, Tassi N, Fontinha D, Bouzón-Arnáiz I, Ferraz R, Araújo MJ, Fernàndez-Busquets X, Prudêncio M, Gomes P, Teixeira C, (2021). 4,9-Diaminoacridines and 4-Aminoacridines as Dual-Stage Antiplasmodial Hits Chemmedchem 16, 788-792
© 2020 Wiley-VCH GmbH 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.
JTD Keywords: acridines, antimalarial activity, blood-stage, liver-stage, malaria, plasmodium, Acridines, Antimalarial activity, Blood-stage, Liver-stage, Malaria, Plasmodium, Synthesis