A prodrug approach towards the development of tricyclic-based FBPase inhibitors.
Bioorg Med Chem Lett
; 20(9): 2938-41, 2010 May 01.
Article
em En
| MEDLINE
| ID: mdl-20359891
ABSTRACT
For the purpose of reducing the strong CYP3A4 inhibitory potency of diamide prodrug 4, cyclic prodrugs of tricyclic-based FBPase inhibitors were synthesized. Extensive SAR studies led to the discovery of pyridine-containing cyclic prodrug 20, which strongly inhibited glucose production in monkey hepatocytes and also showed weak CYP3A4 inhibitory potency.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Piridinas
/
Tiazóis
/
Pró-Fármacos
/
Alanina
/
Inibidores Enzimáticos
/
Organofosfonatos
/
Inibidores do Citocromo P-450 CYP3A
Limite:
Animals
Idioma:
En
Revista:
Bioorg Med Chem Lett
Ano de publicação:
2010
Tipo de documento:
Article