Discovery and investigation of a novel class of thiophene-derived antagonists of the human glucagon receptor.
Bioorg Med Chem Lett
; 15(5): 1401-5, 2005 Mar 01.
Article
em En
| MEDLINE
| ID: mdl-15713396
ABSTRACT
A novel class of antagonists of the human glucagon receptor (hGCGR) has been discovered. Systematic modification of the lead compound identified substituents that were essential for activity and those that were amenable to further optimization. This SAR exploration resulted in the synthesis of 13, which exhibited good potency as an hGCGR functional antagonist (IC50 = 34 nM) and moderate bioavailability (36% in mice).
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Tiofenos
/
Receptores de Glucagon
Limite:
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Ano de publicação:
2005
Tipo de documento:
Article