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- W3201884022 abstract "Parkinson's disease (PD) is the second most common neurodegenerative disorder. Early diagnosis is the key to treatment but is still a great challenge in the clinic now. The discovery of alpha-synuclein (α-syn) aggregates ligands has become an attractive strategy to meet the early diagnosis of PD. Herein, we designed and synthesized a series of styrylaniline derivatives as novel α-syn aggregates ligands. Several compounds displayed good potency to α-syn aggregates with Kd values less than 0.1 μM. The docking study revealed that the hydrogen bonds and cation-pi interaction between ligands and α-syn aggregates would be crucial for the activity. The representative compound 7-16 not only detected α-syn aggregates in both SH-SY5Y cells and brain tissues prepared from two kinds of α-syn preformed-fibrils-injected mice models but also showed good blood-brain barrier penetration characteristics in vivo with a brain/plasma ratio over 1.0, which demonstrates its potential as a lead compound for further development of in vivo imaging agents." @default.
- W3201884022 created "2021-10-11" @default.
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- W3201884022 date "2021-12-01" @default.
- W3201884022 modified "2023-09-23" @default.
- W3201884022 title "Discovery of styrylaniline derivatives as novel alpha-synuclein aggregates ligands" @default.
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- W3201884022 doi "https://doi.org/10.1016/j.ejmech.2021.113887" @default.
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