2026-04-04T02:26:21Zhttps://recercat.cat/oai/requestoai:recercat.cat:2445/2262332026-03-20T15:48:34Zcom_2072_1057col_2072_478902col_2072_478905col_2072_478917
RECERCAT
author
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
2026-01-27T13:13:14Z2026-01-27T13:13:14Z2024-04-152026-01-15T14:28:16Z
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.
cc-by-nc-nd (c) Fonte, Mélanie et al., 2024 https://creativecommons.org/licenses/by-nc-nd/4.0/ info:eu-repo/semantics/openAccess
Antireumàtics
Medicaments anticolesterolèmics
Coenzims
Antirheumatic agents
Anticholesteremic agents
Coenzymes
Disclosure of cinnamic acid/4,9-diaminoacridine conjugates as multi-stage antiplasmodial hits
info:eu-repo/semantics/article info:eu-repo/semantics/publishedVersion