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
en 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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Base de datos:
MEDLINE
Asunto principal:
Tiofenos
/
Receptores de Glucagón
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2005
Tipo del documento:
Article