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Abstract
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A series of novel tetrahydropyrimidin-4-yl)pyridine derivatives 6(a–h)
have been designed and synthesized as inhibitors of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). The chemical structures of
all newly synthesized compounds were characterized by spectroscopic
methods (IR, 1H NMR, 13C NMR) and elemental analyzes. The in vitro
studies showed that all the synthesized derivatives showed significant
BChE inhibitory activity more potent than donepezil as the standard
(IC50 values less than 0.1 mM). All the target compounds demonstrated
good AChE inhibitory effects comparable with donepezil as the reference drug with IC50 values ranging from 0.08 to 0.1 mM. The best
results were obtained by 4-methyl substituted derivative 6d with IC50
value of 0.082 mM which was comparable with AChE inhibitory effects
of donepezil (IC50 ¼ 0.079 mM).
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