Journal
CHEMMEDCHEM
Volume 16, Issue 5, Pages 788-792Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/cmdc.202000740
Keywords
acridines; antimalarial activity; blood-stage; liver-stage; malaria; Plasmodium; synthesis
Categories
Funding
- Fundacao para a Ciencia e Tecnologia (FCT, Portugal) [UIDB/50006/2020, PTDC/BTM-SAL/29786/2017, PTDC/SAU-INF/29550/2017]
- Spanish Ministry of Science, Innovation and Universities [RTI2018-094579-B-I00]
- Generalitat de Catalunya, Spain [2017-SGR-908]
- FCT [SFRH/BD/147345/2019]
- Fundação para a Ciência e a Tecnologia [SFRH/BD/147345/2019, PTDC/SAU-INF/29550/2017] Funding Source: FCT
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Two novel acridine-based compound families, combining features of primaquine and chloroquine, have shown dual-stage antiplasmodial activity against both chloroquine-sensitive and -resistant Plasmodium falciparum strains, as well as against Plasmodium berghei.
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.
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