Synthesis and activity of N-cyanoguanidine-piperazine P2X7 antagonists

被引：10

作者：

Betschmann, Patrick ^{[1
]}

Bettencourt, Brian ^{[1
]}

Donnelly-Roberts, Diana ^{[1
]}

Friedman, Michael ^{[1
]}

George, Jonathan ^{[1
]}

Hirst, Gavin ^{[1
]}

Josephsohn, Nathan ^{[1
]}

Konopacki, Donald ^{[1
]}

Li, Biqin ^{[1
]}

Maull, John ^{[1
]}

Morytko, Michael J. ^{[1
]}

Moore, Nigel StJohn ^{[1
]}

Namovic, Marian ^{[1
]}

Rafferty, Paul ^{[1
]}

Salmeron-Garcia, Jose-Andres ^{[1
]}

Tarcsa, Edit ^{[1
]}

Wang, Lu ^{[1
]}

Woller, Kevin ^{[1
]}

机构：

[1] Abbott Biores Ctr, Dept Med Chem, Worcester, MA 01605 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 14期

关键词：

P2X7; antagonists; cyanoguanidine; piperazine;

D O I：

10.1016/j.bmcl.2008.06.055

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel series of cyanoguanidine-piperazine P2X(7) antagonists were identified and structure-activity relationship (SAR) studies described. Compounds were assayed for activity at human and rat P2X(7) receptors in addition to their ability to inhibit IL-1 beta release from stimulated human whole blood cultures. Compound 27 possesses potent activity (0.12 mu M) in this latter assay and demonstrates moderate clearance in-vivo. (C) 2008 Elsevier Ltd. All rights reserved.

引用

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页码：3848 / 3851

页数：4

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