AI Article Synopsis
- Current treatments for Alzheimer's disease are mainly limited to acetylcholinesterase inhibitors and memantine, which target specific pathways.
- Emerging multi-target ligands, like ladostigil and others, show promise as they offer multiple therapeutic benefits beyond just enzyme inhibition, including cognitive enhancement and antioxidant effects.
- These new compounds also provide protection against oxidative stress and regulate critical processes related to Alzheimer's pathology, suggesting a broader approach to treatment might be on the horizon.
Article Abstract
Current options for the treatment of Alzheimeŕs disease have been restricted to prescription of acetylcholinesterase inhibitors or N-methyl-d-aspartate receptor antagonist, memantine. Propargylamine-derived multi-target directed ligands, such as ladostigil, M30, ASS234 and contilisant, involve different pathways. Apart from acting as inhibitors of both cholinesterases and monoamine oxidases, they show improvement of cognitive impairment, antioxidant activities, enhancement of iron-chelating activities, protect against tau hyperphosphorylation, block metal-associated oxidative stress, regulate APP and Aβ expression processing by the non-amyloidogenic α-secretase pathway, suppress mitochondrial permeability transition pore opening, and coordinate protein kinase C signaling and Bcl-2 family proteins. Other hybrid propargylamine derivatives are also reported.
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| http://dx.doi.org/10.1016/j.bmcl.2019.126880 | DOI Listing |
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