Abstract
A series of 2-(4-phenylpiperazin-1-yl)pyrimidine-5-carboxamide derivatives as acetylcholinesterase inhibitors (AChEIs) were designed and synthesized for the treatment of Alzheimer’s disease (AD). Their bioactivities were evaluated by the Ellman’s method, and the results showed that most of synthesized compounds displayed moderate acetylcholinesterase inhibitory activities in vitro. Among them, compound 6g exhibited the most potent inhibitory activity against AChE with IC50 of 0.90 μM, and poor inhibitory activity against butyrylcholinesterase (BuChE) with IC50 of 7.53 μM, which indicated that compound 6g was a selective AChE inhibitor, and compound 6g as a selective AChE inhibitor was confirmed by the molecular docking studies of compound 6g with AChE and BuChE. Furthermore, the mechanism of inhibition of compound 6g against AChE was analyzed by the kinetic study, and the result indicated that compound 6g was the mixed-type inhibitor of competitive inhibition and non-competitive inhibition. All the above showed that compound 6g could be considered as a lead compound for the development of AD drugs.
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