BACE-1 inhibitory activities of new substituted phenyl-piperazine coupled to various heterocycles:: Chromene, coumarin and quinoline

被引：55

作者：

Garino, C ^{[1
]}

Pietrancosta, N ^{[1
]}

Laras, Y ^{[1
]}

Moret, V ^{[1
]}

Rolland, A ^{[1
]}

Quéléver, G ^{[1
]}

Kraus, JL ^{[1
]}

机构：

[1] Univ Mediterrannee, Fac Sci Luminy, Lab Chim Biomol, INSERM,U263,IBDM, F-13288 Marseille 09, France

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 07期

关键词：

inhibitors; beta-secretase; Alzheimer's disease; phenyl-piperazine; heterocycles;

D O I：

10.1016/j.bmcl.2005.12.064

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The protease beta-secretase plays a central role in the synthesis of pathogenic amyloid-beta in Alzheimer's disease. Here, we report a new series of analogues based on the phenyl-piperazine scaffold coupled to various heterocyclic moieties, which demonstrate improved inhibitory activities on BACE-1 (FRET assay) compared to already known naphthyl counterparts. The obtained results suggest further structural modifications to access to more potent BACE-1 inhibitors. (C) 2006 Elsevier Ltd. All rights reserved.

引用

页码：1995 / 1999

页数：5

共 21 条

[1] NON-CATALYZED REDUCTIONS WITH FORMATE SALTS - CONVERSION OF NITROAROMATIC COMPOUNDS TO THE CORRESPONDING PRIMARY AMINES [J].