1.
Bioorg Med Chem Lett
; 13(24): 4385-8, 2003 Dec 15.
Artículo
en Inglés
| MEDLINE
| ID: mdl-14643331
RESUMEN
The preparation of a series of substituted indoles coupled to six- and seven-membered cyclic lactams is described and their role as human glycogen phosphorylase a inhibitors discussed. The SAR of the indole moiety and lactam ring are presented.
Asunto(s)
Inhibidores Enzimáticos/farmacología , Glucógeno Fosforilasa/antagonistas & inhibidores , Quinolinas/síntesis química , Quinolinas/farmacología , Inhibidores Enzimáticos/síntesis química , Inhibidores Enzimáticos/química , Humanos , Cinética , Modelos Moleculares , Conformación Molecular , Quinolinas/química , Relación Estructura-Actividad
2.
Glucose-lowering in a db/db mouse model by dihydropyridine diacid glycogen phosphorylase inhibitors.
Bioorg Med Chem Lett
; 13(20): 3405-8, 2003 Oct 20.
Artículo
en Inglés
| MEDLINE
| ID: mdl-14505637
RESUMEN
The synthesis of a series of novel dihdyropyridine diacid glycogen phosphorylase inhibitors is presented. SAR and functional assay data are discussed, along with the effect of a single inhibitor on blood glucose in a diabetic animal model.
