Amino acid anthranilamide derivatives as a new class of glycogen phosphorylase inhibitors.
Bioorg Med Chem Lett
; 18(14): 4068-71, 2008 Jul 15.
Article
em En
| MEDLINE
| ID: mdl-18554908
ABSTRACT
A series of amino acid anthranilamide derivatives identified from a high-throughput screening campaign as novel, potent, and glucose-sensitive inhibitors of human liver glycogen phosphorylase a are described. A solid-phase synthesis using Wang resin was also developed which provided efficient access to a variety of analogues, and resulted in the identification of key structure-activity relationships, and the discovery of a potent exemplar (IC(50)=80 nM). The SAR scope, synthetic strategy, and in vitro results for this series are presented herein.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Glicogênio Fosforilase Hepática
/
Ortoaminobenzoatos
Limite:
Animals
/
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Ano de publicação:
2008
Tipo de documento:
Article