Abstract
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, Aβ 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).
Keywords: Coumarin, Alzheimer´s Disease, acetylcholinesterase inhibitor, Aβ aggregation, bis-coumarin dimers, tacrine-coumarin heterodimers, monoamine oxidases.
Graphical Abstract
Call for Papers in Thematic Issues
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