Please use this identifier to cite or link to this item: http://hdl.handle.net/2445/211262
Title: New 4-(N-cinnamoylbutyl)aminoacridines as potential multi-stage antiplasmodial leads
Author: Fonte, Mélanie
Fontinha, Diana
Moita, Diana
Caño Prades, Omar
Avalos Padilla, Yunuen
Fernàndez Busquets, Xavier
Prudêncio, Miguel
Gomes, Paula
Teixeira, Cátia
Keywords: Plasmodium falciparum
Farmacologia
Plasmodium falciparum
Pharmacology
Issue Date: 5-Oct-2023
Publisher: Elsevier
Abstract: 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.
Note: Reproducció del document publicat a: https://doi.org/10.1016/j.ejmech.2023.115575
It is part of: European Journal Of Medicinal Chemistry, 2023, num. 258
URI: http://hdl.handle.net/2445/211262
Related resource: https://doi.org/10.1016/j.ejmech.2023.115575
ISSN: 1768-3254
Appears in Collections:Articles publicats en revistes (Institut de Nanociència i Nanotecnologia (IN2UB))
Articles publicats en revistes (ISGlobal)
Articles publicats en revistes (Institut de Bioenginyeria de Catalunya (IBEC))

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