1609078-46-7Relevant articles and documents
Multi-target-oriented protective agent neurocyte
-
, (2017/03/28)
PROBLEM TO BE SOLVED: To provide a promising multi target direction type pharmaceutical candidate molecule which is promising for treatments of Alzheimer-type dementia (AD), which is a molecule having good cell membrane permeability including blood brain barrier.SOLUTION: A compound designed by a conjunction method with which a benzylpiperidine part of an acetylcholine esterase (AChE) inhibitor, donepezil is connected through an oligomethylene linker and combined with a propargyl part having a monoamine oxidase(MAO) inhibition activity and 8-hydroxy-5-methylaminoquinoline functional group, i.e. a center nitrogen atom substituted by a pro-chelator motif of a biochemical metal, interacts with AChE and butyrylcholinesterase(BuChE), further MAOA and B.
Neuroprotective multi-target directed drugs
-
Paragraph 0100; 0105, (2014/05/20)
A new family of multitarget molecules able to interact with acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE), as well as with monoamino oxidase (MAO) A and B, has been synthesized. Novel compounds have been designed using a conjunctive approach that combines the benzylpiperidine moiety of the AChE inhibitor donepezil, connected through an oligomethylene linker, to a central nitrogen atom substituted with the propargyl moiety responsible for the MAO inhibition, and a 8-hydroxy-5-methylaminoquinoline functional group, the biometal pro-chelator motif. Overall, the results suggest that the new compounds are promising multitarget drug candidates with potencial impact for AD therapy.