Synthesis, Crystal Structure and Cholinesterase Enzymes Inhibitory Activities of New Pyridine Alkaloid Derivative

摘要

A new pyridine alkaloid derivative named as 2-(6-benzyl-4-oxo-5-phenyl-1,4-dihydro pyridine-3-yl)-benzoic acid ethylester (3) has been prepared by the reaction of ninhydrin with 1,3-diphenylacetone p-tosylhydrazone and the structure has been established with the help of spectral analysis and X-ray analysis. The title compound demonstrated potent inhibitory activity against butyrylcholinesterase (BChE; IC_(50) = 4.91 uM) comparable to physostigmine (IC_(50) = 4.72 x 10~(-1) μM). However it showed moderate inhibitory activity against acetylcholinesterase (AChE; IC_(50) = 82.00 μM)). It was BChE selective over AChE, in contrast to physostigmine, which was more AChE selective. Being a potent and selective BChE inhibitor, it may serve as a new class of drug for prevention of the progression of neurodegeneration as well for symptomatic treatment of Alzheimer patient.