Novel and potent tacrine-related hetero- and homobivalent ligands for acetylcholinesterase and butyrylcholinesterase

被引：60

作者：

Savini, L

Campiani, G

Gaeta, A

Pellerano, C

Fattorusso, C

Chiasserini, L

Fedorko, JM

Saxena, A

机构：

[1] Univ Siena, Dipartimento Farmaco Chim Tecnol, I-53100 Siena, Italy

[2] Univ Salerno, Dipartimento Sci Farmaceut, I-84084 Fisciano, Italy

[3] Univ Naples Federico II, Dipartimento Chim Sostanze Nat, I-80131 Naples, Italy

[4] Walter Reed Forest Glen Annex, Div Biochem, Silver Spring, MD 20910 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 13期

关键词：

D O I：

10.1016/S0960-894X(01)00294-3

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Based upon synthetic and biochemical results, a novel and potent tacrine analogue and heterobivalent analogues of tacrine, were designed. The role played by the amino groups of homo- and heterobivalent ligands in the interaction with the peripheral and catalytic sites of AChE and BuChE were investigated. The syntheses of these materials together with the results of AChE/BuChE inhibition assays are detailed. (C) 2001 Elsevier Science Ltd. All rights reserved.

引用

页码：1779 / 1782

页数：4

共 15 条

[1] Evaluation of short-tether bis-THA AChE inhibitors. A further test of the dual binding site hypothesis [J].