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Cage amines as the stopper inhibitors of cholinesterases.

Abstract：

: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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Lin G,Tsai HJ,Tsai YH

doi

10.1016/s0960-894x(03)00599-7

subject

Has Abstract

pub_date

2003-09-01 00:00:00

pages

2887-90

issue

17

eissn

0960-894X

issn

1464-3405

pii

S0960894X03005997

journal_volume

13

pub_type

杂志文章

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