Synthesis and structure-activity relationship (SAR) studies of 1,2,3-triazole, amide, and ester-based benzothiazole derivatives as potential molecular probes for tau protein

Hendris Wongso, Maiko Ono, Tomoteru Yamasaki, Katsushi Kumata, Makoto Higuchi, Ming Rong Zhang, Michael J. Fulham, Andrew Katsifis, Paul A. Keller

研究成果: ジャーナルへの寄稿学術論文査読

5 被引用数 (Scopus)

抄録

The pyridinyl-butadienyl-benzothiazole (PBB3 15) scaffold was used to develop tau ligands with improved in vitro and in vivo properties for imaging applications to provide insights into the etiology and characteristics of Alzheimer's disease. The photoisomerisable trans-butadiene bridge of PBB3 was replaced with 1,2,3-triazole, amide, and ester moieties and in vitro fluorescence staining studies revealed that triazole derivatives showed good visualisation of Aβ plaques, but failed to detect the neurofibrillary tangles (NFTs) in human brain sections. However, NFTs could be observed using the amide 110 and ester 129. Furthermore, the ligands showed low to high affinities (Ki = >1.5 mM-0.46 nM) at the shared binding site(s) with PBB3.

本文言語英語
ページ(範囲)858-868
ページ数11
ジャーナルRSC Medicinal Chemistry
14
5
DOI
出版ステータス出版済み - 27-01-2023
外部発表はい

All Science Journal Classification (ASJC) codes

  • 生化学
  • 分子医療
  • 薬理学
  • 薬科学
  • 創薬
  • 有機化学

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