Snythesis and structure-activity relationships of indole and benzimidazole piperazines as histamine H4 receptor antagonists

被引：114

作者：

Terzioglu, N

van Rijn, RM

Bakker, RA

De Esch, IJP

Leurs, R

机构：

[1] Free Univ Amsterdam, Fac Chem, Dept Pharmacochem, Div Med Chem,LACDR, NL-1081 HV Amsterdam, Netherlands

[2] Univ Istanbul, Fac Pharm, Dept Pharmaceut Chem, TR-34452 Istanbul, Turkey

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 21期

关键词：

histamine H-4 receptor; antagonists;

D O I：

10.1016/j.bmcl.2004.08.035

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We describe the structure-activity relationships for a series of ligands structurally related to the recently identified (5-chloro-1H-indol-2-yl)-(4-methyl-piperazin-1-yl)-methanone (1) as histamine H-4 receptor (H4R) antagonists. Furthermore we identified related benzimidazoles as novel lead compounds for the H4R. The ligands have been evaluated by radioligand displacement studies and functional assays for their interaction with both the human histamine H-3 and H-4 receptors and exhibit pK(i) values up to 7.5 at the human H4R. (C) 2004 Elsevier Ltd. All rights reserved.

引用

页码：5251 / 5256

页数：6

共 34 条

[1]

ASHTON MJ, 1984, J MED CHEM, V27, P1245, DOI 10.1021/jm00376a002

[2] Indole amide derivatives:: synthesis, structure-activity relationships and molecular modelling studies of a new series of histamine H1-receptor antagonists [J].