Discovery of diarylurea P2Y(1) antagonists with improved aqueous solubility.
Bioorg Med Chem Lett
; 23(11): 3239-43, 2013 Jun 01.
Article
em En
| MEDLINE
| ID: mdl-23602442
ABSTRACT
Preclinical data suggests that P2Y1 antagonists, such as diarylurea compound 1, may provide antithrombotic efficacy similar to P2Y12 antagonists and may have the potential of providing reduced bleeding liabilities. This manuscript describes a series of diarylureas bearing solublizing amine side chains as potent P2Y1 antagonists. Among them, compounds 2l and 3h had improved aqueous solubility and maintained antiplatelet activity compared with compound 1. Compound 2l was moderately efficacious in both rat and rabbit thrombosis models and had a moderate prolongation of bleeding time in rats similar to that of compound 1.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Compostos de Fenilureia
/
Piridinas
/
Ureia
/
Receptores Purinérgicos P2Y1
/
Antagonistas do Receptor Purinérgico P2Y
/
Fibrinolíticos
Limite:
Animals
/
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2013
Tipo de documento:
Article
País de afiliação:
Estados Unidos