Discovery of potent and orally active tricyclic-based FBPase inhibitors.
Bioorg Med Chem
; 18(14): 5346-51, 2010 Jul 15.
Article
em En
| MEDLINE
| ID: mdl-20542703
ABSTRACT
With the aim of exploring the effect of tricyclic-based FBPase inhibitors in cells and in vivo, a series of prodrugs of tricyclic phosphonates was designed and synthesized. Introducing prodrug moieties into tricyclic-based phosphonates led to the discovery of prodrug 15c, which strongly inhibited glucose production in monkey hepatocytes. Furthermore, prodrug 15c lowered blood glucose levels in fasted cynomolgus monkeys.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Pró-Fármacos
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Frutose-Bifosfatase
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Organofosfonatos
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Glucose
Idioma:
En
Ano de publicação:
2010
Tipo de documento:
Article