Synthesis of novel histamine H4 receptor antagonists

被引：19

作者：

Lane, Charlotte A. L. ^{[1
]}

Hay, Duncan ^{[1
]}

Mowbray, Charles E. ^{[1
]}

Paradowski, Michael ^{[1
]}

Selby, Matthew D. ^{[1
]}

Swain, Nigel A. ^{[1
]}

Williams, David H. ^{[1
]}

机构：

[1] Pfizer Worldwide Res & Dev, Worldwide Med Chem, Sandwich CT13 9NJ, Kent, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2012年 / 22卷 / 02期

关键词：

Histamine; Azaindole; Bicyclic; Amidine; Isostere; H-4; RECEPTOR; PHARMACOLOGICAL CHARACTERIZATION; LIGAND EFFICIENCY; CLONING; DISCOVERY; POTENT; ANTIHISTAMINES; BENZIMIDAZOLE; EXPRESSION; RESPONSES;

D O I：

10.1016/j.bmcl.2011.11.098

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

This letter describes the discovery and synthesis of a series of octahydropyrrolo[3,4-c]pyrrole based selective histamine hH4 receptor antagonists. The amidine compound 20 was found to be a potent and selective histamine H4 receptor antagonist with moderate clearance and a high volume of distribution. (C) 2011 Elsevier Ltd. All rights reserved.

引用

页码：1156 / 1159

页数：4

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