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

• Main Authors: Zofia Chrienova (Author), Eugenie Nepovimova (Author), Rudolf Andrys (Author), Rafael Dolezal (Author), Jana Janockova (Author), Lubica Muckova (Author), Lenka Fabova (Author), Ondrej Soukup (Author), Patrik Oleksak (Author), Martin Valis (Author), Jan Korabecny (Author), José Marco-Contelles (Author), Kamil Kuca (Author)
• Format: Book
• Published: Taylor & Francis Group, 2022-12-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.

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, c...