Pyrrolo(iso)quinoline derivatives as 5-HT2C receptor agonists

被引：21

作者：

Adams, DR ^{[1
]}

Bentley, JM ^{[1
]}

Benwell, KR ^{[1
]}

Bickerdike, MJ ^{[1
]}

Bodkin, CD ^{[1
]}

Cliffe, IA ^{[1
]}

Dourish, CT ^{[1
]}

George, AR ^{[1
]}

Kennett, GA ^{[1
]}

Knight, AR ^{[1
]}

Malcolm, CS ^{[1
]}

Mansell, HL ^{[1
]}

Misra, A ^{[1
]}

Quirk, K ^{[1
]}

Roffey, JRA ^{[1
]}

Vickers, SP ^{[1
]}

机构：

[1] Vernalis Plc, Wokingham RG41 5UA, Berks, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 03期

关键词：

obesity; serotonin; 5-HT2C; agonist;

D O I：

10.1016/j.bmcl.2005.10.029

中图分类号：

R914 [药物化学];

学科分类号：

100701 [药物化学];

摘要：

A series of 1-(1-pyrrolo(iso)quinolinyl)-2-propylamines was synthesised and evaluated as 5-HT2C receptor agonists for the treatment of obesity. The general methods of synthesis of the precursor indoles are described. The functional efficacy and radioligand binding data for the compounds at 5-HT2 receptor subtypes are reported. The analogue which showed the highest 5-HT2C binding affinity (27, 1.6 nM) was found to be successful in reducing food intake in rats. (c) 2005 Elsevier Ltd. All rights reserved.

引用

页码：677 / 680

页数：4

共 28 条

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THE REACTION OF VINYL GRIGNARD-REAGENTS WITH 2-SUBSTITUTED NITROARENES - A NEW APPROACH TO THE SYNTHESIS OF 7-SUBSTITUTED INDOLES [J].