Discovery of potent and selective adamantane-based small-molecule P2X7 receptor antagonists/interleukin-1β,6 inhibitors

被引：58

作者：

Furber, Mark

Alcaraz, Lilian

Bent, Janice E.

Beyerbach, Armin

Bowers, Keith

Braddock, Martin

Caffrey, Moya V.

Cladingboel, David

Collington, John

Donald, David K.

Fagura, Malbinder

Ince, Frank

Kinchin, Elizabeth C.

Laurent, Celine

Lawson, Mandy

Luker, Timothy J.

Mortimore, Michael M. P.

Pimm, Austen D.

Riley, Robert J.

Roberts, Nicola

Robertson, Mark

Theaker, Jill

Thorne, Philip V.

Weaver, Richard

Webborn, Peter

Willis, Paul

机构：

[1] AstraZeneca R&D Charnwood, Dept Med Chem, Loughborough LE11 5RH, Leics, England

[2] AstraZeneca R&D Charnwood, Dept Discovery Biosci, Loughborough LE11 5RH, Leics, England

[3] AstraZeneca R&D Charnwood, Dept Phys & Metab Sci, Loughborough LE11 5RH, Leics, England

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2007年 / 50卷 / 24期

关键词：

INTERLEUKIN-1; ANTAGONIST; DERIVATIVES; MECHANISMS; ANAKINRA; RELEASE; EXPRESS; TARGET; CELLS; ATP;

D O I：

10.1021/jm700949w

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：

A novel series of antagonists of the human P2X(7) receptor is describcd Modification of substituents enabled identification of compounds selective for the rat P2X(7) receptor and provides useful pharmacological tools for evaluation of the role of P2X(7) in disease.

引用

页码：5882 / 5885

页数：4

共 25 条

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Mechanisms of inhibition of collagen-induced arthritis by murine IL-18 binding protein [J].