2. Academic Validation
  3. Inhibitory properties of quinopimaric acid derivatives towards cholinesterases

Inhibitory properties of quinopimaric acid derivatives towards cholinesterases

  • Nat Prod Res. 2023 Oct 9:1-9. doi: 10.1080/14786419.2023.2266107.
Elena Tretyakova 1,  Niels V Heise 2,  René Csuk 2,  Oxana Kazakova 1
Affiliations

Affiliations

  • 1 Ufa Institute of Chemistry of the Ufa Federal Research Centre of the Russian Academy of Sciences, Ufa, Russian Federation.
  • 2 Martin-Luther-University Halle-Wittenberg, Halle (Saale), Germany.
PMID: 37812150 DOI: 10.1080/14786419.2023.2266107
Abstract

A series of new diterpene quinopimaric acid derivatives modified at the hydroxyl group with different pharmacophore fragments has been synthesised and their (along with previously obtained compounds) inhibitory properties towards cholinesterases were studied. Thereby an indole-3-acetyl derivative 7 and a propargyl substituted compound 28 were shown to be excellent and acetylcholinesterase-selective inhibitors. Both compounds inhibited the Enzyme as a mixed type inhibitor, and Ki values of 0.41 and 0.44 µM and Ki' values of 0.98 and 2.26 µM were determined. The binding interactions between all active compounds and ligands protein were confirmed through molecular docking study.

Keywords

Abietane diterpenoids; acetylcholinesterase; butyrylcholinesterase; diene adduct; levopimaric acid; quinopimaric acid.

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