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4,9‐Diaminoacridines and 4‐Aminoacridines as Dual‐Stage Antiplasmodial Hits
Author(s) -
Fonte Mélanie,
Tassi Natália,
Fontinha Diana,
BouzónArnáiz Inés,
Ferraz Ricardo,
Araújo Maria J.,
FernàndezBusquets Xavier,
Prudêncio Miguel,
Gomes Paula,
Teixeira Cátia
Publication year - 2021
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.202000740
Subject(s) - primaquine , plasmodium berghei , plasmodium falciparum , chloroquine , plasmodium (life cycle) , malaria , acridine , pharmacology , drug resistance , antimalarial agent , drug discovery , biology , chemistry , parasite hosting , biochemistry , immunology , microbiology and biotechnology , genetics , computer science , world wide web
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.