Benzimidazolone-based serotonin 5-HT1A or 5-HT7R ligands: Synthesis and biological evaluation

被引：25

作者：

Badarau, Eduard ^{[1
,2
]}

Suzenet, Franck ^{[1
]}

Bojarski, Andrzej J. ^{[3
]}

Finaru, Adriana-Luminita ^{[2
]}

Guillaumet, Gerald ^{[1
]}

机构：

[1] Univ Orleans, CNRS, UMR 6005, UFR Sci,Inst Chim Organ & Analyt, F-45067 Orleans 2, France

[2] Univ Bacau Calea Marasesti, Bacau 600115, Romania

[3] Polish Acad Sci, Inst Pharmacol, PL-31343 Krakow, Poland

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 06期

关键词：

Benzimidazolone; 5-HT(7)Rs Ligands; Arylpiperazines; PROTEIN-COUPLED RECEPTOR; HIGH-AFFINITY; ANTAGONIST SB-269970; CRYSTAL-STRUCTURE; PHARMACOPHORE; ARYLPIPERAZINE; INTERLEUKIN-6; DERIVATIVES; SELECTIVITY; DEPRESSION;

D O I：

10.1016/j.bmcl.2009.02.008

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A new group of serotoninergic 5-HT1A or 5-HT7 receptor ligands was identified. These compounds were designed and synthesized on a benzimidazolone scaffold and they enrich the well-known arylpiperazine class of 5-HT ligands. Diverse pharmacomodulations induced a shift in the affinity and selectivity pro. le with final identification of new potent hits. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：1600 / 1603

页数：4

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