Identification of 2-arylbenzimidazoles as potent human histamine H4 receptor ligands

被引：45

作者：

Lee-Dutra, Alice ^{[1
]}

Arienti, Kristen L. ^{[1
]}

Buzard, Daniel J. ^{[1
]}

Hack, Michael D. ^{[1
]}

Khatuya, Haripada ^{[1
]}

Desai, Pragnya J. ^{[1
]}

Nguyen, Steven ^{[1
]}

Thurmond, Robin L. ^{[1
]}

Karlsson, Lars ^{[1
]}

Edwards, James P. ^{[1
]}

Breitenbucher, J. Guy ^{[1
]}

机构：

[1] Johnson & Johnson Pharmaceut Res & Dev, LLC, San Diego, CA 92121 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 23期

关键词：

histamine H-4; arylbenzimidazole;

D O I：

10.1016/j.bmcl.2006.08.117

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 2-arylbenzimidazoles was synthesized and found to bind with high affinity to the human histamine H-4 receptor. Structure-activity relationships were investigated through library preparation and evaluation as well as traditional medicinal chemistry approaches, leading to the discovery of compounds with single-digit nanomolar affinity for the H-4 receptor. (c) 2006 Elsevier Ltd. All rights reserved.

引用

页码：6043 / 6048

页数：6

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