Potent acetylcholinesterase inhibitors: Design, synthesis, and structure-activity relationships of bis-interacting ligands in the galanthamine series

被引：103

作者：

Mary, A ^{[1
]}

Renko, DZ ^{[1
]}

Guillou, C ^{[1
]}

Thal, C ^{[1
]}

机构：

[1] CNRS, Inst Chim Subst Nat, F-91198 Gif Sur Yvette, France

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 1998年 / 6卷 / 10期

关键词：

D O I：

10.1016/S0968-0896(98)00133-3

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

New galanthamine derivatives, especially bis-interacting ligands 3-5 and 7-9 were prepared in order to interact with the catalytic and the peripheral sites of acetylcholinesterase (AChE). The synthesis, the anticholinesterase activities, and the structure-activity relationships of bis-interacting ligands are reported. Compounds 4d-e were found to be more potent than galanthamine and tacrine in inhibiting AChE. (C) 1998 Elsevier Science Ltd. All rights reserved.

引用

页码：1835 / 1850

页数：16

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