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Premium Phthalimide‐Derived N ‐Benzylpyridinium Halides Targeting Cholinesterases: Synthesis and Bioactivity of New Potential Anti‐Alzheimer's Disease Agents
Author(s)
Saeedi Mina,
Golipoor Maedeh,
Mahdavi Mohammad,
Moradi Alireza,
Nadri Hamid,
Emami Saeed,
Foroumadi Alireza,
Shafiee Abbas
Publication year2016
Publication title
archiv der pharmazie
Resource typeJournals
PublisherWiley-Blackwell
In order to develop potent dual‐binding cholinesterase inhibitors as potential drugs for the treatment of Alzheimer's disease, we designed and synthesized phthalimide‐based acetylcholinesterase (AChE) inhibitors ( 7 ) containing a substituted N ‐benzylpyridinium residue. The in vitro anti‐cholinesterase assay employing the target compounds against AChE and butyrylcholinesterase (BChE) revealed the 2‐fluorobenzylpyridinium derivative 7d as the most potent compound against both enzymes, with IC 50 values of 0.77 and 8.71 μM. The docking study of compound 7d into the active site of AChE showed the gorge‐spanning binding mode, in which the compound spans the narrow hydrophobic gorge from the bottom to the rim.
Subject(s)acetylcholinesterase , aché , biochemistry , butyrylcholinesterase , chemistry , cholinesterase , combinatorial chemistry , docking (animal) , enzyme , ic50 , in vitro , medicine , nursing , pharmacology , phthalimide , stereochemistry
Language(s)English
SCImago Journal Rank0.468
H-Index61
eISSN1521-4184
pISSN0365-6233
DOI10.1002/ardp.201500425

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