Hitting drug-resistant malaria infection with triazole-linked flavonoid-chloroquine hybrid compounds.
Future Med Chem
; 14(24): 1865-1880, 2022 12.
Article
em En
| MEDLINE
| ID: mdl-36622669
ABSTRACT
Background:
Malaria represents the major parasitic disease in tropical regions, and the development of new potent drugs is of pivotal importance. In this study, a series of hybrid molecules were designed by linking the 7-chloroquinoline core of chloroquine to different fluorinated flavonoid-related scaffolds. Materials &methods:
Compounds were prepared by exploiting the click chemistry approach, allowing the introduction of a 1,2,3-triazole, a privileged structural motif in antiparasitic dug discovery.Results:
Compounds 1b and 1c were the most interesting and were endowed with the highest in vitro activity, mainly against a resistant Plasmodium falciparum strain. They also inhibited hemozoin formation, and 1c was more effective than chloroquine against stage V gametocytes.Conclusion:
The homoisoflavone core is a new, promising antimalarial scaffold that deserves further investigation.Palavras-chave
Texto completo:
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Base de dados:
MEDLINE
Assunto principal:
Malária
/
Antimaláricos
Limite:
Humans
Idioma:
En
Ano de publicação:
2022
Tipo de documento:
Article