4,9-Diaminoacridines and 4-Aminoacridines as Dual-Stage Antiplasmodial Hits

• Type: Article in International Scientific Journal
• Date: 2021

Authors

Fonte, M (Author) Other; Tassi, N (Author) Other; Fontinha, D (Author) Other; Bouzon Arnaiz, I (Author) Other; Ferraz, R (Author) Other; Maria J Araujo (Author) FCUP; Fernandez Busquets, X (Author) Other; Prudencio, M (Author) Other; Paula Gomes (Author) FCUP; Catia Teixeira (Author) FCUP

Journal

Title: ChemMedChem

Vol. 16

Pages: 788-792

ISSN: 1860-7179

Publisher: Wiley-Blackwell

Indexing

ISI Web of Knowledge - 5 Citations

Scopus - 5 Citations

Other information

Authenticus ID: P-00T-32D

DOI: 10.1002/cmdc.202000740

Abstract (EN): Multi-stage drugs have been prioritized in antimalarial drug discovery, as targeting more than one process in the Plasmodium life cycle is likely to increase efficiency, while decreasing the chances of emergence of resistance by the parasite. Herein, we disclose two novel acridine-based families of compounds that combine the structural features of primaquine and chloroquine. Compounds prepared and studied thus far retained the in vitro activity displayed by the parent drugs against the erythrocytic stages of chloroquine-sensitive and -resistant Plasmodium falciparum strains, and against the hepatic stages of Plasmodium berghei, hence acting as dual-stage antiplasmodial hits.

Language: English

Type (Professor's evaluation): Scientific

No. of pages: 5