Potent P2Y1 urea antagonists bearing various cyclic amine scaffolds.
Bioorg Med Chem Lett
; 23(24): 6825-8, 2013 Dec 15.
Article
em En
| MEDLINE
| ID: mdl-24269480
ABSTRACT
A number of new amine scaffolds with good inhibitory activity in the ADP-induced platelet aggregation assay have been found to be potent antagonists of the P2Y1 receptor. SAR optimization led to the identification of isoindoline 3c and piperidine 4a which showed good in vitro binding and functional activities, as well as improved aqueous solubility. Among them, the piperidine 4a showed the best overall profile with favorable PK parameters.
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Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Ureia
/
Receptores Purinérgicos P2Y1
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Agonistas do Receptor Purinérgico P2Y
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Aminas
Limite:
Animals
/
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Ano de publicação:
2013
Tipo de documento:
Article