Synthesis and biological evaluation of thieno[3,2-c]pyrazol-3-amine derivatives as potent glycogen synthase kinase 3β inhibitors for Alzheimer's disease

N Yan, XL Shi, LQ Tang, DF Wang, X Li… - Journal of Enzyme …, 2022 - Taylor & Francis
Glycogen synthase kinase 3β (GSK-3β) catalyses the hyperphosphorylation of tau protein in
the Alzheimer's disease (AD) pathology. A series of novel thieno [3, 2-c] pyrazol-3-amine …

Synthesis and biological evaluation of thieno [3, 2-c] pyrazol-3-amine derivatives as potent glycogen synthase kinase 3β inhibitors for Alzheimer's disease

N Yan, F Xie, LQ Tang, DF Wang, X Li, C Liu… - Bioorganic Chemistry, 2023 - Elsevier
Glycogen synthase kinase 3β (GSK-3β) is a potential target for anti-Alzheimer's disease
(AD) drug development. In this study, a series of novel thieno [3, 2-c] pyrazol-3-amine …

Design, synthesis and structure–activity relationships of 1, 3, 4-oxadiazole derivatives as novel inhibitors of glycogen synthase kinase-3β

M Saitoh, J Kunitomo, E Kimura, Y Hayase… - Bioorganic & medicinal …, 2009 - Elsevier
Glycogen synthase kinase-3β (GSK-3β) is implicated in abnormal hyperphosphorylation of
tau protein and its inhibitors are expected to be a promising therapeutic agents for the …

Discovery of novel potent and highly selective glycogen synthase kinase-3β (GSK3β) inhibitors for Alzheimer's disease: design, synthesis, and characterization of …

S Berg, M Bergh, S Hellberg, K Högdin… - Journal of medicinal …, 2012 - ACS Publications
Glycogen synthase kinase-3β, also called tau phosphorylating kinase, is a proline-directed
serine/threonine kinase which was originally identified due to its role in glycogen …

Discovery of novel α‐carboline derivatives as glycogen synthase kinase‐3β inhibitors for the treatment of Alzheimer's disease

H Chen, C Yu, W Liu, C Zhu, X Jiang, C Xu… - Archiv der …, 2022 - Wiley Online Library
Alzheimer's disease (AD) is a chronic and progressive neurodegenerative disease,
characterized by irreversible cognitive impairment, memory loss, and behavioral …

[HTML][HTML] Virtual screening and testing of GSK-3 inhibitors using human SH-SY5Y cells expressing Tau folding reporter and mouse hippocampal primary culture under …

CH Lin, YS Hsieh, YC Sun, WH Huang… - Biomolecules & …, 2023 - ncbi.nlm.nih.gov
Glycogen synthase kinase-3β (GSK-3β) is an important serine/threonine kinase that
implicates in multiple cellular processes and links with the neurodegenerative diseases …

A novel glycogen synthase kinase‐3 inhibitor 2‐methyl‐5‐(3‐{4‐[(S )‐methylsulfinyl]phenyl}‐1‐benzofuran‐5‐yl)‐1,3,4‐oxadiazole decreases tau phosphorylation …

T Onishi, H Iwashita, Y Uno, J Kunitomo… - Journal of …, 2011 - Wiley Online Library
J. Neurochem.(2011) 10.1111/j. 1471‐4159.2011. 07532. x Abstract Alzheimer's disease
(AD) is a neurodegenerative disorder leading to a progressive loss of cognitive function and …

Discovery of novel quinolin-2-one derivatives as potential GSK-3β inhibitors for treatment of Alzheimer's disease: Pharmacophore-based design, preliminary SAR, in …

EA Moustafa, HA Allam, MA Fouad, AM El Kerdawy… - Bioorganic …, 2024 - Elsevier
Recently, glycogen synthase kinase-3β (GSK-3β) has been considered as a critical factor
implicated in Alzheimer's disease (AD). In a previous work, a 3D pharmacophore model for …

2-{3-[4-(Alkylsulfinyl) phenyl]-1-benzofuran-5-yl}-5-methyl-1, 3, 4-oxadiazole derivatives as novel inhibitors of glycogen synthase kinase-3β with good brain …

M Saitoh, J Kunitomo, E Kimura… - Journal of medicinal …, 2009 - ACS Publications
Glycogen synthase kinase 3β (GSK-3β) inhibition is expected to be a promising therapeutic
approach for treating Alzheimer's disease. Previously we reported a series of 1, 3, 4 …

Discovery of novel 2-(4-aryl-2-methylpiperazin-1-yl)-pyrimidin-4-ones as glycogen synthase kinase-3β inhibitors

T Kohara, K Nakayama, K Watanabe, S Kusaka… - Bioorganic & Medicinal …, 2017 - Elsevier
We herein describe the results of further evolution of glycogen synthase kinase (GSK)-3β
inhibitors from our promising compounds containing a 3-methylmorpholine moiety …