Synthesis and evaluation of a 2-benzothiazolylphenylmethyl ether class of histamine H4 receptor antagonists

被引：5

作者：

Labeeuw, Olivier ^{[1
]}

Levoin, Nicolas ^{[1
]}

Billot, Xavier ^{[1
]}

Danvy, Denis ^{[1
,2
]}

Calmels, Thierry ^{[1
]}

Krief, Stephane ^{[1
]}

Ligneau, Xavier ^{[1
]}

Berrebi-Bertrand, Isabelle ^{[1
]}

Robert, Philippe ^{[1
]}

Lecomte, Jeanne-Marie ^{[1
]}

Schwartz, Jean-Charles ^{[1
]}

Capet, Marc ^{[1
]}

机构：

[1] Bioprojet Biotech, 4 Rue Chesnay Beauregard,BP 96205, F-35762 St Gregoire, France

[2] Fac Sci & Tech, Interor, IRCOF, UMR CNRS LFAOC 6014, 1 Rue Tesniere, F-76821 Mont St Aignan, France

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2016年 / 26卷 / 21期

关键词：

Histamine; Histamine H4 receptor; Asthma; Atopic dermatitis; H-4; RECEPTOR; HIGH-AFFINITY; LIGANDS; CLONING; ANALOGS; H3;

D O I：

10.1016/j.bmcl.2016.09.049

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Synthesis and biological evaluation of a new class of histamine H-4 receptor ligands, distinct from the previously reported chemotypes, are described. A virtual screening of our corporate compound collection identified a hit with an undesired dual H3R/H4R activity. Chemical exploration led to the discovery of a more potent and selective 2-benzothiazolylphenylmethyl ether lead compound. (C) 2016 Elsevier Ltd. All rights reserved.

引用

页码：5263 / 5266

页数：4

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