Privileged multi-target directed propargyl-tacrines combining cholinesterase and monoamine oxidase inhibition activities.

ABSTRACT: Twenty-four novel compounds bearing tetrahydroacridine and N-propargyl moieties have been designed, synthesised, and evaluated in vitro for their anti-cholinesterase and anti-monoamine oxidase activities. Propargyltacrine 23 (IC₅₀ = 21 nM) was the most potent acetylcholinesterase (AChE) inhibitor, compound 20 (IC₅₀ = 78 nM) showed the best inhibitory human butyrylcholinesterase (hBChE) profile, and ligand 21 afforded equipotent and significant values on both ChEs (human AChE [hAChE]: IC₅₀ = 0.095 ± 0.001 µM; hBChE: IC₅₀ = 0.093 ± 0.003 µM). Regarding MAO inhibition, compounds 7, 15, and 25 demonstrated the highest inhibitory potential towards hMAO-B (IC₅₀

SUBMITTER: Chrienova Z 

PROVIDER: S-EPMC9518283 | biostudies-literature | 2022 Dec

REPOSITORIES: biostudies-literature