Potent 4-aminopiperidine based antimalarial agents.
Bioorg Med Chem Lett
; 15(2): 345-8, 2005 Jan 17.
Article
em En
| MEDLINE
| ID: mdl-15603951
ABSTRACT
A series of compounds with potent activity against a multi-drug-resistant strain of Plasmodium falciparum, the causative agent of the deadliest strain of malaria, is described. These compounds were also tested for cytotoxicity in human foreskin fibroblast assays, evaluated to determine their logD, and assayed for metabolism by human and murine hepatocytes. This work resulted in the development of compounds 9e and 10d, which showed good potency (IC(50)=75 nM and <60 nM, respectively, against Dd2), acceptable logD values, and reasonable metabolic stability.
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Base de dados:
MEDLINE
Assunto principal:
Piperidinas
/
Plasmodium falciparum
/
Hepatócitos
/
Antimaláricos
Limite:
Animals
/
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2005
Tipo de documento:
Article
País de afiliação:
Estados Unidos