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…

Index: Martinez, Ana; Alonso, Mercedes; Castro, Ana; Perez, Concepcion; Moreno, Francisco J. Journal of Medicinal Chemistry, 2002 , vol. 45, # 6 p. 1292 - 1299

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Citation Number: 373

Abstract

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 ...