1.
Bioorg Med Chem Lett
; 23(13): 3983-7, 2013 Jul 01.
Artigo
em Inglês
| MEDLINE
| ID: mdl-23683591
RESUMO
New potent glycogen synthase kinase-3 (GSK-3) inhibitors, 8-amino-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one derivatives, were designed by modeling, synthesized and evaluated in vitro. Compound 17c showed good potency in enzyme and cell-based assays (IC50=111 nM, EC50=1.78 µM). Moreover, it has demonstrated desirable water solubility, PK profile, and moderate brain penetration.