Synthesis and evaluation of pyrazine and quinoxaline fluorophores for in vivo detection of cerebral tau tangles in Alzheimer's models

Biyue Zhu; Ting Zhang; Qian Jiang; Ying Li; Yu Fu; Jiapei Dai; Ge Li; Qingrong Qi; Yan Cheng

doi:10.1039/c8cc06897f

Synthesis and evaluation of pyrazine and quinoxaline fluorophores for in vivo detection of cerebral tau tangles in Alzheimer's models

Chem Commun (Camb). 2018 Oct 11;54(82):11558-11561. doi: 10.1039/c8cc06897f.

Authors

Biyue Zhu¹, Ting Zhang, Qian Jiang, Ying Li, Yu Fu, Jiapei Dai, Ge Li, Qingrong Qi, Yan Cheng

Affiliation

¹ Key Laboratory of Drug-Targeting and Drug Delivery System of the Education Ministry, Sichuan Engineering Laboratory for Plant-Sourced Drug and Sichuan Research Center for Drug Precision Industrial Technology, West China School of Pharmacy, Sichuan University, Chengdu, 610041, China. yancheng@scu.edu.cn qiqinrong@scu.edu.cn.

PMID: 30204164
DOI: 10.1039/c8cc06897f

Abstract

A series of pyrazine and quinoxaline probes (QNNs) were synthesized and evaluated. The quinoxaline derivative 3b, with high affinity and selectivity for tau aggregates, favorable fluorescence turn-on capability and brain kinetics, was successfully applied to the detection of tau tangles both in vitro and in mice in vivo.

MeSH terms

Aged
Alzheimer Disease / diagnostic imaging*
Animals
Brain / diagnostic imaging*
Cell Line, Tumor
Fluorescent Dyes / chemistry*
Humans
Male
Mice, Transgenic
Optical Imaging / methods*
Pyrazines / chemistry*
Quinoxalines / chemistry*
tau Proteins / analysis*

Substances

Fluorescent Dyes
Pyrazines
Quinoxalines
tau Proteins