Please use this identifier to cite or link to this item: http://hdl.handle.net/11455/69743
標題: Benzene-1,2-, 1,3-, and 1,4-di-N-substituted carbamates as conformationally constrained inhibitors of acetylcholinesterase
作者: Lin, M.C.
Hwang, M.T.
Chang, H.G.
Lin, C.S.
Lin, G.
關鍵字: acetylcholinesterase
carbamate
conformation
inhibitor
structure-reactivity relationships
pancreatic cholesterol esterase
butyrylcholinesterase
cholinesterases
recognition
mechanism
site
期刊/報告no:: Journal of Biochemical and Molecular Toxicology, Volume 21, Issue 6, Page(s) 348-353.
摘要: Benzene-1,2-, 1,3-, and 1,4-di-N-substituted carbamates (1-15) are synthesized as the conformationally constrained inhibitors of acetylcholinesterase and mimic gauche, eclipsed, and anti-conforinations of acetylcholine, respectively. All carbamates 1-15 are characterized as the pseudo substrate inhibitors of acetylcholinesterase. For a series of geometric isomers, the inhibitory potencies are as follows: benzene-1,4-di-N-substituted carbamate (para compound)> benzene-1,3-di-N-substituted carbamate (meta compound) > benzene-1,2-di-N-substituted carbarnate (ortho compound). Therefore, benzene1,4-di-N-substituted carbamates (para compounds), with the angle of 180 degrees between two C(benzene)-O bonds, mimic the preferable anti C-O/C-N conformers of acetylcholine for the choline ethylene backbone in the acetylcholinesterase catalysis. (c) 2007 Wiley Periodicals, Inc.
URI: http://hdl.handle.net/11455/69743
ISSN: 1095-6670
文章連結: http://dx.doi.org/10.1002/jbt.20202
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