Novel sulfonamides having dual dopamine D2 and D3 receptor affinity show in vivo antipsychotic efficacy with beneficial cognitive and EPS profile

被引：16

作者：

Agai-Csongor, Eva ^{[1
]}

Nogradi, Katalin ^{[1
]}

Galambos, Janos ^{[1
]}

Vago, Istvan ^{[1
]}

Bielik, Attila ^{[1
]}

Magdo, Ildiko ^{[1
]}

Ignacz-Szendrei, Gyoergyi ^{[1
]}

Keseru, Gyoergy Miklos ^{[1
]}

Greiner, Istvan ^{[1
]}

Laszlovszky, Istvan ^{[1
]}

Schmidt, Eva ^{[1
]}

Kiss, Bela ^{[1
]}

Saghy, Katalin ^{[1
]}

Laszy, Judit ^{[1
]}

Gyertyan, Istvan ^{[1
]}

Zajer-Balazs, Maria ^{[1
]}

Gemesi, Larisza ^{[1
]}

Domany, Gyoergy ^{[1
]}

机构：

[1] Gedeon Richter Chem Works Ltd, H-1475 Budapest, Hungary

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 19期

关键词：

arylsulfonamides; dopamine D3 and D2 ligands; antipsychotic; cognition enhancer;

D O I：

10.1016/j.bmcl.2007.08.015

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel series of arylsulfonamides was prepared either by automated parallel or by traditional solution-phase synthesis. Several members of this compound library were identified as high-affinity dopamine D3 and D2 receptor ligands. The most interesting representative, compound 2, showed potent antipsychotic behaviour coupled with a beneficial cognitive and EPS profile. (C) 2007 Elsevier Ltd. All rights reserved.

引用

页码：5340 / 5344

页数：5