Abstrakt
Coumarins are naturally occurring phytochemicals with heterocyclic structures which display a wide range of biological activities against neurological diseases such as Alzheimer's disease (AD). This study reviews recent research into the design, synthesis and pharmacological profile of several series of synthetic coumarin ligands with clearcholinesterase, and assesses the monoamino oxidases (MAO-A and MAO-B) inhibitory activity, A beta anti-aggregation potency and antioxidant properties reported for these novel derivatives.
Our attention is focused on a comparison of the neuroprotective effects of these coumarin derivatives in terms of their potential as mono-, homo-and heterodimers as agents in the treatment of AD. The monocoumarin derivatives 13a & 13b with benzyl pyridinium group showed outstanding levels of acetylcholinesterase inhibitory activity (IC50 = 0.11, 0.16 nM).
Bis-coumarin ligands showed high levels of inhibitory activity and selectivity for MAO-A. Tacrinecoumarin heterodimer 21b was the most active inhibitor of hBChE (IC50 = 38 pM).