Design, synthesis, and SAR analysis of novel selective σ1 ligands

被引：30

作者：

Collina, Siniona

Loddo, Guya

Urbano, Mariangela

Linati, Laura

Callegari, Athos

Ortuso, Francesco

Alcaro, Stefano

Laggner, Christian

Langer, Thierry

Prezzavento, Orazio

Ronsisvalle, Giuseppe

Azzolina, Ornella

机构：

[1] Univ Pavia, Dipartimento Chim Farmaceut, I-27100 Pavia, Italy

[2] Univ Pavia, Ctr Grandi Strumenti, I-27100 Pavia, Italy

[3] Univ Pavia, Dipartimento Sci Terra, I-27100 Pavia, Italy

[4] Univ Catanzaro Magna Graecia, Dipartimento Sci Farmacol Compleso Nini Barbieri, I-88021 Roccelletta Di Borgia, CZ, Italy

[5] Univ Innsbruck, Dept Pharmaceut Chem, A-6020 Innsbruck, Austria

[6] Univ Innsbruck, Ctr Mol Biosci CMBI, A-6020 Innsbruck, Austria

[7] Univ Catania, Dipartimento Sci Farmaceut, I-95125 Catania, Italy

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2007年 / 15卷 / 02期

关键词：

arylalkylamines; sigma receptors; molecular modeling; SAR studies;

D O I：

10.1016/j.bmc.2006.10.048

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：

A new series of arylalkyl- and alkenylamines was designed, synthesized, and evaluated for binding to sigma(1) and sigma(2) receptors. Many compounds exhibited nanomolar affinity for sigma(1) subtype receptor with good selectivity over sigma(2). A molecular modeling study was conducted in order to rationalize the experimental data, and the structure-receptor affinities are discussed. (c) 2006 Elsevier Ltd. All rights reserved.

引用

页码：771 / 783

页数：13

共 34 条

[1] Chemical and biological profile of racemic and optically active dialkylaminoalkylnaphthalenes with analgesic activity [J].