Novel tricyclic quinazolinimines and related tetracyclic nitrogen bridgehead compounds as cholinesterase inhibitors with selectivity towards butyrylcholinesterase

被引：94

作者：

Decker, M ^{[1
]}

Krauth, F ^{[1
]}

Lehmann, J ^{[1
]}

机构：

[1] Univ Jena, Inst Pharm, Lehrstuhl Pharmazeut Med Chem, D-07743 Jena, Germany

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2006年 / 14卷 / 06期

关键词：

cholinesterase inhibition; tricyclic[2,1-b]quinazolinimines; Ellman's assay; butyrylcholinesterase (BChE) selectivity;

D O I：

10.1016/j.bmc.2005.10.044

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 [生物化学与分子生物学]; 081704 [应用化学];

摘要：

Tetracyclic nitrogen bridgehead compounds, dibenzodiazecines and tricyclic quinazolinimines, in which the size of the alicyclic ring system and the length of the alkyl chain between the quinazolinimine moiety and a phenyl ring connected to the inline nitrogen atom were changed systematically, were synthesized and their ability to inhibit acetyl- and butyrylcholinesterase (AChE/BChE), respectively, was evaluated. Moderate and strong inhibitors of BChE-compared to galanthamine and rivastigmine-were identified, which show mixed affinities or are moderately or highly selective towards BChE, respectively. (c) 2005 Elsevier Ltd. All rights reserved.

引用

页码：1966 / 1977

页数：12

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