Discovery of a series of 6,7-dimethoxy-4-pyrrolidylquinazoline PDE10A inhibitors.
J Med Chem
; 50(2): 182-5, 2007 Jan 25.
Article
em En
| MEDLINE
| ID: mdl-17228859
ABSTRACT
A papaverine based pharmacophore model for PDE10A inhibition was generated via SBDD and used to design a library of 4-amino-6,7-dimethoxyquinazolines. From this library emerged an aryl ether pyrrolidyl 6,7-dimethoxyquinazoline series that became the focal point for additional modeling, X-ray, and synthetic efforts toward increasing PDE10A inhibitory potency and selectivity versus PDE3A/B. These efforts culminated in the discovery of 29, a potent and selective brain penetrable inhibitor of PDE10A.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Inibidores de Fosfodiesterase
/
Pirrolidinas
/
Quinazolinas
/
Diester Fosfórico Hidrolases
Limite:
Animals
Idioma:
En
Revista:
J Med Chem
Ano de publicação:
2007
Tipo de documento:
Article