Discovery of a novel series of CXCR3 antagonists

被引：15

作者：

Crosignani, Stefano ^{[1
]}

Missotten, Marc ^{[1
]}

Cleva, Christophe ^{[1
]}

Dondi, Ruggero ^{[1
]}

Ratinaud, Yann ^{[1
]}

Humbert, Yves ^{[1
]}

Mandal, Ashis Baran ^{[2
]}

Bombrun, Agnes ^{[1
]}

Power, Christine ^{[1
]}

Chollet, Andre ^{[1
]}

Proudfoot, Amanda ^{[1
]}

机构：

[1] Merck Serono SA, CH-1202 Geneva, Switzerland

[2] Syngene Int Ltd, Bangalore 560099, Karnataka, India

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 12期

关键词：

CXCR3; Chemokines; GPCR antagonists; Rheumatoid arthritis; Multiple sclerosis; CENTRAL-NERVOUS-SYSTEM; MULTIPLE-SCLEROSIS; T-CELLS; CHEMOKINE RECEPTORS; LIGANDS; EXPRESSION;

D O I：

10.1016/j.bmcl.2010.04.113

中图分类号：

R914 [药物化学];

学科分类号：

100705 [微生物与生化药学];

摘要：

The discovery of a novel series of CXCR3 antagonists is described. Starting from an HTS positive, iterative optimization gave potent compounds (IC(50) 15 nM in a chemotaxis assay). The strategy employed to improve the metabolic stability of these derivatives is described. (C) 2010 Elsevier Ltd. All rights reserved.

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收藏

页码：3614 / 3617

页数：4

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