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Publication
4,9‐Diaminoacridines and 4‐Aminoacridines as dual‐stage antiplasmodial hits
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Advisor(s)
Abstract(s)
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.
Description
© 2020 Wiley-VCH GmbH
Keywords
Plasmodium Acridines Antimalarial activity Blood-stage Liver-stage Malaria Synthesis
Pedagogical Context
Citation
ChemMedChem. 2021 Mar 3;16(5):788-792
Publisher
Wiley