108655-56-7Relevant articles and documents
Synthesis and evaluation of novel GSK-3β inhibitors as multifunctional agents against Alzheimer's disease
Shi, Xiao-Long,Wu, Jing-De,Liu, Ping,Liu, Zhao-Peng
, p. 211 - 225 (2019)
To target the multi-facets of Alzheimer's disease (AD), a series of novel GSK-3β inhibitors containing the 2,3-diaminopyridine moiety were designed and synthesized. The amide derivatives 5a-f showed moderate potency against GSK-3β with weak Cu2+, Zn2+ and Al3+ chelating ability. The imine derivatives 9a, 9b and 9e were potent GSK-3β inhibitors and selective Cu2+and Al3+ chelators. The 1,2-diamine derivatives 10a-e were strong metal-chelators, but decreased or lost their GSK-3β inhibitory potency. In vitro, compounds 9a, 9b and 9e, especially 9b, exhibited good Cu2+-induced Aβ aggregation inhibition, Cu2+-Aβ complex disaggregation, ROS formation inhibition, and antioxidant activities. In cells, compounds 9a, 9b and 9e can inhibit tau protein phosphorylation and protect neuro cells against Cu2+-Aβ1–42 and H2O2-induced cell damage. Furthermore, compound 9b was predicted to have the ability to pass the BBB with drug likeness properties. Therefore, compound 9b might be a good lead for the development of novel GSK-3β inhibitors targeting multi-facets of AD.
SUBSTITUTED-QUINOXALINE-TYPE-PIPERIDINE COMPOUNDS AND THE USES THEREOF
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Page/Page column 169, (2009/04/25)
The invention relates to Substituted-Quinoxaline-Type Piperidine Compounds, compositions comprising an effective amount of a Substituted-Quinoxaline-Type Piperidine Compound and methods to treat or prevent a condition, such as pain, comprising administeri
HETEROCYCLIC-SUBSTITUTED PIPERDINE COMPOUNDS AND THE USES THEREOF
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Page/Page column 243, (2008/12/07)
The invention relates to Heterocyclic-Substituted Piperidine Compounds, compositions comprising an effective amount of a Heterocyclic-Substituted Piperidine Compound and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of a Heterocyclic-Substituted Piperidine Compound
Applications of 1-Alkoxycarbonyl- and 1-Acyl-v-triazolopyridines as Acylating Reagents
Torrini, Ines,Zecchini, Giampiero Pagani,Agrosi, Francesco,Paradisi, Mario Paglialunga
, p. 1459 - 1463 (2007/10/02)
Selective N-protection of hydroxyamino esters has been readily achieved using 1-alkoxycarbonyl- or 1-acyl-v-triazolopyridines.The amide-type triazolides reacted with alcohols in the presence of DBU at room temperature to afford in high yields the corresponding esters.The different reactivity of 1- and 3-alkoxycarbonyl derivatives of the title bicyclic system toward primary amines has been further investigated.