Discovery of XEN445: a potent and selective endothelial lipase inhibitor raises plasma HDL-cholesterol concentration in mice.
Bioorg Med Chem
; 21(24): 7724-34, 2013 Dec 15.
Article
em En
| MEDLINE
| ID: mdl-24211162
ABSTRACT
Endothelial lipase (EL) activity has been implicated in HDL metabolism and in atherosclerotic plaque development; inhibitors are proposed to be efficacious in the treatment of dyslipidemia related cardiovascular disease. We describe here the discovery of a novel class of anthranilic acids EL inhibitors. XEN445 (compound 13) was identified as a potent and selective EL inhibitor, that showed good ADME and PK properties, and demonstrated in vivo efficacy in raising plasma HDLc concentrations in mice.
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Base de dados:
MEDLINE
Assunto principal:
Pirrolidinas
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Benzoatos
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Inibidores Enzimáticos
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Descoberta de Drogas
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Lipase
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HDL-Colesterol
Idioma:
En
Ano de publicação:
2013
Tipo de documento:
Article