1,2-Diphenoxiethane salts as potent antiplasmodial agents.
Bioorg Med Chem Lett
; 28(14): 2485-2489, 2018 08 01.
Article
em En
| MEDLINE
| ID: mdl-29880399
ABSTRACT
In this article we present a series of non-cytotoxic potent human choline kinase (CK) inhibitors that exhibit nanomolar antiplasmodial activity in vitro. The most active antiplasmodial compounds, 10a-b, bearing a pyridinium cationic head were inactive against CK, while compounds 10g and 10j with a quinolinium moiety exhibit moderate inhibition of both the parasite and the enzyme. The results point towards an additional mechanism of action unrelated to CK inhibition that remains to be established.
Palavras-chave
Texto completo:
1
Bases de dados:
MEDLINE
Assunto principal:
Plasmodium falciparum
/
Compostos de Bifenilo
/
Colina Quinase
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Inibidores de Proteínas Quinases
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Etano
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Antimaláricos
Limite:
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2018
Tipo de documento:
Article
País de afiliação:
Espanha