New 4-(N-cinnamoylbutyl)aminoacridines as potential multi-stage antiplasmodial leads

• Type: Article in International Scientific Journal
• Date: 2023

Authors

Fonte, M (Author) Other; Fontinha, D (Author) Other; Moita, D (Author) Other; Cano Prades, O (Author) Other; Avalos Padilla, Y (Author) Other; Fernandez Busquets, X (Author) Other; Prudencio, M (Author) Other; Paula Gomes (Author) FCUP; Catia Teixeira (Author) FCUP

Journal

Title: European Journal of Medicinal Chemistry

Vol. 258

ISSN: 0223-5234

Publisher: Elsevier

Indexing

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Other information

Authenticus ID: P-00Y-MTF

DOI: 10.1016/j.ejmech.2023.115575

Abstract (EN): 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 falcip-arum, 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.

Language: English

Type (Professor's evaluation): Scientific

No. of pages: 9