Preparation of piperazine derivatives as 5-HT7 receptor antagonists

被引：29

作者：

Yoon, Juhee ^{[1
]}

Yoo, Eun A. ^{[1
]}

Kim, Ji-Yeon ^{[1
]}

Pae, Ae Nim ^{[2
]}

Rhim, Hyewhon ^{[2
]}

Park, Woo-Kyu ^{[3
]}

Kong, Jae Yang ^{[3
]}

Choo, Hea-Young Park ^{[1
]}

机构：

[1] Ewha Womans Univ, Sch Pharm, Seoul 120750, South Korea

[2] Korea Inst Sci & Technol, Biochem Res Ctr, Seoul 130650, South Korea

[3] Korea Res Inst Chem Technol, Pharmaceut Screening Res Team, Taejon 305343, South Korea

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2008年 / 16卷 / 10期

关键词：

5-HT7 receptor antagonists; piperazine; sulfonamide; 5-HT2c receptor antagonists;

D O I：

10.1016/j.bmc.2008.04.023

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：

Twenty-four compounds of 4-methoxy-N-[3-(4-substituted phenyl-piperazine-1-yl) propyl] benzene sulfonamides and N-[3-(4- substituted phenyl-piperazine-1-yl) propyl] naphthyl sulfonamides were prepared and evaluated as 5-HT7 receptor antagonists. Most of the compounds showed the IC50 values of 12-580 nM. Four methyl branched analogues were also obtained, but the activity for methyl branched analogues was almost same as its straight chain congeners. Among the synthesized compounds, 3c showed a good activity on 5-HT7 receptors and a good selectivity on 5-HT1a, 5-HT2a, 5-HT2c, and 5-HT6 receptors. (C) 2008 Elsevier Ltd. All rights reserved.

引用

页码：5405 / 5412

页数：8

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