Discovery and optimization of 2-aryl oxazolo-pyrimidines as adenosine kinase inhibitors using liquid phase parallel synthesis

被引：36

作者：

Bauser, M

Delapierre, G

Hauswald, M

Flessner, T

D'Urso, D

Hermann, A

Beyreuther, B

De Vry, J

Spreyer, P

Reissmüller, E

Meier, H

机构：

[1] Bayer Health Care, Division Pharma, Medicinal Chemistry

[2] Bayer Health Care, Division Pharma, CNS Research

[3] CEA/LETI, Biol. and Hlth. Care Syst. Dept., Grenoble

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 08期

关键词：

D O I：

10.1016/j.bmcl.2004.01.082

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Adeno sine kinase inhibition is an attractive therapeutic approach for several conditions for example, neurodegeneration, seizures, ischemia, inflammation and pain. Several nucleosidic and non-nucleosidic inhibitors are available. Using a virtual screening approach, we have discovered that 2-aryl oxazolo-pyrimidines are adenosine kinase inhibitors. Subsequent high throughput derivatization enabled the optimization of this new inhibitor chemotype resulting in highly potent derivatives. A variety of analogues were produced by applying liquid phase parallel synthesis to vary the 7-amino residues as well as the 2-aryl moiety. (C) 2004 Elsevier Ltd. All rights reserved.

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页码：1997 / 2000

页数：4

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