First non-ATP competitive glycogen synthase kinase 3 β (GSK-3β) inhibitors: thiadiazolidinones (TDZD) as potential drugs for the treatment of Alzheimer's disease
A Martinez, M Alonso, A Castro, C Pérez…
文献索引:Martinez, Ana; Alonso, Mercedes; Castro, Ana; Perez, Concepcion; Moreno, Francisco J. Journal of Medicinal Chemistry, 2002 , vol. 45, # 6 p. 1292 - 1299
Glycogen synthase kinase 3 β (GSK-3β) has a central role in Alzheimer's disease (AD). Selective inhibitors which avoid τ hyperphosphorylation may represent an effective therapeutical approach to the AD pharmacotherapy and other neurodegenerative disorders. Here, we describe the synthesis, biological evaluation, and SAR of the small heterocyclic thiadiazolidinones (TDZD) as the first non-ATP competitive inhibitor of GSK-3β. Their ...