2. Academic Validation
  3. The total synthesis of berberine and selected analogues, and their evaluation as amyloid beta aggregation inhibitors

The total synthesis of berberine and selected analogues, and their evaluation as amyloid beta aggregation inhibitors

  • Eur J Med Chem. 2021 Apr 5:215:113289. doi: 10.1016/j.ejmech.2021.113289.
Misato Tajiri 1,  Ryo Yamada 1,  Mayumi Hotsumi 1,  Koki Makabe 1,  Hiroyuki Konno 2
Affiliations

Affiliations

  • 1 Graduate School of Science and Engineering, Yamagata University, Yonezawa, Yamagata 992-8510, Japan.
  • 2 Graduate School of Science and Engineering, Yamagata University, Yonezawa, Yamagata 992-8510, Japan. Electronic address: konno@yz.yamagata-u.ac.jp.
PMID: 33611188 DOI: 10.1016/j.ejmech.2021.113289
Abstract

The total synthesis of berberine and selected analogues. And their evaluation as amyloid β (Aβ) aggregation inhibitors is described. The key step in the synthesis, the assembly of the berberine framework, was accomplished using an intermolecular Heck reaction. Berberine analog 17 incorporating a tertiary amine moiety showed good anti Aβ aggregation activity, water solubility, and almost no toxicity to nerve cells.

Keywords

Aggregation inhibition; Alzheimer’s disease; Amyloid beta; Berberine.

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