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
收藏
页码：771 / 783
页数：13
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