Design, synthesis and assay of 2-(4-phenylpiperazin-1-yl)pyrimidine-5- carboxamide derivatives as acetylcholinesterase inhibitors
نویسندگان
چکیده
A series of 2-(4-phenylpiperazin-1-yl)pyrimidine-5-carboxamide derivatives as acetylcholinesterase inhibitors (AChEIs) were designed and synthesized for the treatment Alzheimer’s disease (AD). Their bioactivities evaluated by Ellman’s method, results showed that most compounds displayed moderate inhibitory activities in vitro. Among them, compound 6g exhibited potent activity against AChE with IC50 0.90 μM, poor butyrylcholinesterase (BuChE) 7.53 which indicated was a selective inhibitor, inhibitor confirmed molecular docking studies BuChE. Furthermore, mechanism inhibition analyzed kinetic study, result mixed-type competitive non-competitive inhibition. All above could be considered lead development AD drugs.
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ژورنال
عنوان ژورنال: Medicinal Chemistry Research
سال: 2022
ISSN: ['1554-8120', '1054-2523']
DOI: https://doi.org/10.1007/s00044-022-02949-0