Synthesis and SAR of pyrimidine-based, non-nucleotide P2Y14 receptor antagonists.
Bioorg Med Chem Lett
; 21(10): 2832-5, 2011 May 15.
Article
em En
| MEDLINE
| ID: mdl-21507642
ABSTRACT
A weak antagonist of the pyrimidinergic receptor P2Y(14) containing a dihydropyridopyrimidine core was identified through high-throughput screening. Subsequent optimization led to potent, non-UTP competitive antagonists and represent the first reported non-nucleotide antagonists of this receptor. Compound 18q was identified as a 10 nM P2Y(14) antagonist with good oral bioavailability and provided sufficient exposure in mice to be used as a tool for future in vivo studies.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Pirimidinas
/
Receptores Purinérgicos P2
/
Antagonistas do Receptor Purinérgico P2
Limite:
Animals
Idioma:
En
Revista:
Bioorg Med Chem Lett
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2011
Tipo de documento:
Article