Journal
FRONTIERS IN NEUROSCIENCE
Volume 10, Issue -, Pages -Publisher
FRONTIERS MEDIA SA
DOI: 10.3389/fnins.2016.00294
Keywords
multi-target directed ligands; Alzheimer's disease; monoamine oxidases; cholinesterases; drugs
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Funding
- MINECO (Spain) [SAF20112-33304, SAF2015-65586-R]
- EU (COST Action) [1103]
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Highlights: ASS2324 is a hybrid compound resulting from the juxtaposition of donepezil and the propargylamine PF9601N ASS2324 is a multi-target directed propargylamine able to bind to all the AChE/BuChE and MAO NB enzymes ASS2324 shows antioxidant, neuroprotective and suitable permeability properties ASS2324 restores the scopolamine-induced cognitive impairment to the same extent as donepezil, and is less toxic ASS2324 prevents beta-amyloid induced aggregation in the cortex of double transgenic mice ASS2324 is the most advanced anti-Alzheimer agent for pre-clinical studies that we have identified in our laboratories The complex nature of Alzheimer's disease (AD) has prompted the design of Multi-Target-Directed Ligands (MTDL) able to bind to diverse biochemical targets involved in the progress and development of the disease. In this context, we have designed a number of MTD propargylamines (MTDP) showing antioxidant, anti-beta-amyloid, anti-inflammatory, as well as cholinesterase and monoamine oxidase (MAO) inhibition capacities. Here, we describe these properties in the MTDL ASS234, our lead-compound ready to enter in pre-clinical studies for AD, as a new multipotent, permeable cholinesterase/monoamine oxidase inhibitor, able to inhibit A beta-aggregation, and possessing antioxidant and neuroprotective properties.
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