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Si us plau utilitzeu sempre aquest identificador per citar o enllaçar aquest document: https://hdl.handle.net/2445/211262
New 4-(N-cinnamoylbutyl)aminoacridines as potential multi-stage antiplasmodial leads
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A novel family of 4-aminoacridine derivatives was obtained by linking this heteroaromatic core to different trans-cinnamic acids. The 4-(N-cinnamoylbutyl)aminoacridines obtained exhibited in vitro activity in the low- or sub-micromolar range against (i) hepatic stages of Plasmodium berghei, (ii) erythrocytic forms of Plasmodium falciparum, and (iii) early and mature gametocytes of Plasmodium falciparum. The most active compound, having a meta-fluorocinnamoyl group linked to the acridine core, was 20- and 120-fold more potent, respectively, against the hepatic and gametocyte stages of Plasmodium infection than the reference drug, primaquine. Moreover, no cytotoxicity towards mammalian and red blood cells at the concentrations tested was observed for any of the compounds under investigation. These novel conjugates represent promising leads for the development of new multi-target antiplasmodials.Copyright © 2023 The Authors. Published by Elsevier Masson SAS.. All rights reserved.
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FONTE, Mélanie, FONTINHA, Diana, MOITA, Diana, CAÑO PRADES, Omar, AVALOS PADILLA, Yunuen, FERNÀNDEZ BUSQUETS, Xavier, PRUDÊNCIO, Miguel, GOMES, Paula, TEIXEIRA, Cátia. New 4-(N-cinnamoylbutyl)aminoacridines as potential multi-stage antiplasmodial leads. _European Journal Of Medicinal Chemistry_. 2023. Vol. 258. [consulta: 20 de gener de 2026]. ISSN: 1768-3254. [Disponible a: https://hdl.handle.net/2445/211262]