Cage amines as the stopper inhibitors of cholinesterases

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Please use this identifier to cite or link to this item: http://hdl.handle.net/11455/68231

標題:	Cage amines as the stopper inhibitors of cholinesterases
作者:	Lin, G. Tsai, H.J. Tsai, Y.H.
關鍵字:	active-site gorge;human butyrylcholinesterase;acetylcholinesterase;binding;analogs;residues
Project:	Bioorganic & Medicinal Chemistry Letters
期刊/報告no：:	Bioorganic & Medicinal Chemistry Letters, Volume 13, Issue 17, Page(s) 2887-2890.
摘要:	Cage amines 1-4 are potent peripheral anionic site-bound reversible inhibitors of both acetylcholinesterase and butyrylcholinesterase. Cage amines 1-3 are selective butyrylcholinesterase inhibitor versus acetylcholinesterase. For both enzymes, the -log K-i values linearly correlate with the difference of substituted phenyl radius of cage amines (-log K-i = 5.4 + 3.4Deltagamma for acetylcholinesterase, -log K-i = 5.9 + 3.2Deltagamma for butyrylcholinesterase). Moreover, the relationship between the enzymes and cage amines mimics that between bottles and stoppers. (C) 2003 Elsevier Ltd. All rights reserved.
URI:	http://hdl.handle.net/11455/68231
ISSN:	0960-894X
DOI:	10.1016/s0960-894(03)00599-7
Appears in Collections:	期刊論文

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