- 作者: Gialih Lin and Bing-Hong Kao
- 中文摘要: Epoxy type inhibitors, 3-t-butylphenyl 3-1,2-epoxybutyl ether (1), 3-t-butylphenyl 3-1,2-epoxyhexyl ether (2), and 2-naphthyl 3-1,2-epoxyhexyl ether (3) are synthesized as the active site-directed inhibitors of cholesterol esterase, acetylcholinesterase, and butyrylcholinesterase. All epoxy compounds are characterized as the time-independent inhibitors for all three enzymes from the stopped-time assay. Further, all epoxy compounds are characterized as the competitive inhibitors for all three enzymes from the Lineweaver-Burk plots. The inhibition constants (Ki) of cholesterol esterase for compounds 1-3 are 320 40, 190 20, 130 20 M, respectively. The Ki values of acetylcholinesterase for compounds 1-3 are 490 20, 141 5, 200 30 M, respectively. Values of Ki of butyrylcholinesterase for compounds 1-3 are 250 30, 26 4, 120 20 M, respectively. Compound 2 is the most potent inhibitor for butyrylcholinesterase probably because the compound mimics most the natural substrate, butyrylcholine.
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