Synthesis and pharmacology of isoquinuclidine derivatives as 5-HT3 ligands

被引：19

作者：

Iriepa, I

Villasante, FJ

Gálvez, E

Labeaga, L

Innerarity, A

Orjales, A

机构：

[1] Univ Alcala de Henares, Dept Quim Organ, E-28871 Alcala De Henares, Madrid, Spain

[2] FAES SA, Dept Invest, Leioa 48940, Vizcaya, Spain

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 02期

关键词：

D O I：

10.1016/S0960-894X(01)00693-X

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 4-amino-5-chloro-2-methoxybenzoates and benzamides containing the 5- and 6-isoquinuclidinyl system was synthesised and evaluated for binding to 5-HT3, 5-HT4 and D-2 receptors. In general, the isoquinuclidine derivatives at the 5-position have shown to be more potent as 5-HT3 ligands but they also possess 5-HT4 and D-2 properties. However, the results show that the derivatives at the 6-position afforded the most promising compounds in terms of both receptor affinity and selectivity. (C) 2002 Elsevier Science Ltd. All rights reserved.

引用

页码：189 / 192

页数：4

共 15 条

[1] 5-HYDROXYTRYPTAMINE (5-HT3) RECEPTOR ANTAGONISTS .1. INDAZOLE AND INDOLIZINE-3-CARBOXYLIC ACID-DERIVATIVES [J].