Synthesis and biological evaluation of 3-aryltyramines as fragments binding to BACE-1 and BACE-2

被引：12

作者：

Fehler, Stefanie K. ^{[2
]}

Pratsch, Gerald ^{[2
]}

Huber, Walter ^{[1
]}

Gast, Alain ^{[1
]}

Hochstrasser, Remo ^{[1
]}

Hennig, Michael ^{[1
]}

Heinrich, Markus R. ^{[2
]}

机构：

[1] F Hoffmann La Roche & Co Ltd, Discovery Technol, CH-4070 Basel 65319, Switzerland

[2] Univ Erlangen Nurnberg, Dept Chem & Pharm, D-91052 Erlangen, Germany

来源：

TETRAHEDRON LETTERS | 2012年 / 53卷 / 17期

关键词：

Radical reactions; Tyramine; BACE; Biaryl; Arylation; BETA-SECRETASE INHIBITORS; AMYLOID PRECURSOR PROTEIN; CATIONIC PHENYLATION; ALZHEIMERS-DISEASE; ARYLATION; REACTIVITY; CHEMISTRY; ETHERS;

D O I：

10.1016/j.tetlet.2012.02.070

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

3-Aryltyramines were prepared in one single step from tyramine and various arenediazonium salts by radical arylation. Binding as well as enzyme inhibition data of the 14 compounds do not prove true interaction with BACE-1. In contrast, with BACE-2 inhibition and binding could be confirmed indicating that 3-aryltyramines are potential starting points for a drug discovery effort. (c) 2012 Elsevier Ltd. All rights reserved.

引用

页码：2189 / 2194

页数：6

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