2026-04-17T07:38:08Zhttps://recercat.cat/oai/request

oai:recercat.cat:2445/2262332026-04-08T14:28:05Zcom_2072_1057col_2072_478902col_2072_478905col_2072_478917

00925njm 22002777a 4500 dc Fonte, Mélanie author Rôla, Catarina author Santana, Sofia author Avalos Padilla, Yunuen author Fernàndez Busquets, Xavier author Prudêncio, Miguel author Gomes, Paula A. C author Teixeira, Catia Marlene author 2026-01-27T13:13:14Z 2026-01-27T13:13:14Z 2024-04-15 2026-01-15T14:28:16Z 4,9-diaminoacridines with reported antiplasmodial activity were coupled to different trans-cinnamic acids, delivering a new series of conjugates inspired by the covalent bitherapy concept. The new compounds were more potent than primaquine against hepatic stages of Plasmodium berghei, although this was accompanied by cytotoxic effects on Huh-7 hepatocytes. Relevantly, the conjugates displayed nanomolar activities against blood stage P. falciparum parasites, with no evidence of hemolytic effects below 100 mu M. Moreover, the new compounds were at least 25-fold more potent than primaquine against P. falciparum gametocytes. Thus, the new antiplasmodial hits disclosed herein emerge as valuable templates for the development of multi-stage antiplasmodial drug candidates. Antireumàtics Medicaments anticolesterolèmics Coenzims Antirheumatic agents Anticholesteremic agents Coenzymes Disclosure of cinnamic acid/4,9-diaminoacridine conjugates as multi-stage antiplasmodial hits