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Discovery and evaluation of aza-fused tricyclic derivatives for detection of Tau pathology in Alzheimer's disease

Authors :
Tianqing Liu
Yuying Li
Yan Wang
Xiao-Xin Yan
Jiapei Dai
Mengchao Cui
Source :
European Journal of Medicinal Chemistry. 246:114991
Publication Year :
2023
Publisher :
Elsevier BV, 2023.

Abstract

For various neurodegenerative diseases, including Alzheimer's disease (AD), the abnormal aggregation of Tau is not only the predominant contributing factor but also a major biomarker for disease diagnosis. In this study, a series of aza-fused tricyclic derivatives were designed and synthesized. By changing the position and number of nitrogen atoms on the fused tricyclic core, the imidazonaphthyridine scaffold was screened and reported for the first time which could potentially detect Tau aggregates. Through a series of in vitro and in vivo biological evaluations, probe [

Details

ISSN :
02235234
Volume :
246
Database :
OpenAIRE
Journal :
European Journal of Medicinal Chemistry
Accession number :
edsair.doi.dedup.....aec204dd8103b87d5722878cb27c0742
Full Text :
https://doi.org/10.1016/j.ejmech.2022.114991