Discovery of novel N-1 substituted pyrazolopyrimidinones as potent, selective PDE2 inhibitors.
Bioorg Med Chem Lett
; 44: 128082, 2021 07 15.
Article
en En
| MEDLINE
| ID: mdl-33991626
ABSTRACT
A focused SAR study was conducted on a series of N1-substituted pyrazolopyrimidinone PDE2 inhibitors to reveal compounds with excellent potency and selectivity. The series was derived from previously identified internal leads and designed to enhance steric interactions with key amino acids in the PDE2 binding pocket. Compound 26 was identified as a lead compound with excellent PDE2 selectivity and good physicochemical properties.
Palabras clave
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Inhibidores de Fosfodiesterasa
/
Pirazoles
/
Pirimidinonas
/
Fosfodiesterasas de Nucleótidos Cíclicos Tipo 2
/
Descubrimiento de Drogas
Límite:
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2021
Tipo del documento:
Article
Pais de publicación:
ENGLAND
/
ESCOCIA
/
GB
/
GREAT BRITAIN
/
INGLATERRA
/
REINO UNIDO
/
SCOTLAND
/
UK
/
UNITED KINGDOM