Synthesis and in vitro activity of N′-cyano-4-(2-phenylacetyl)-N-o-tolylpiperazine-1-carboximidamide P2X7 antagonists

被引：15

作者：

Morytko, Michael J. ^{[2
]}

Betschmann, Patrick ^{[2
]}

Woller, Kevin ^{[2
]}

Ericsson, Anna ^{[2
]}

Chen, Haipeng ^{[2
]}

Donnelly-Roberts, Diana L. ^{[1
]}

Namovic, Marian T. ^{[1
]}

Jarvis, Michael F. ^{[1
]}

Carroll, William A. ^{[1
]}

Rafferty, Paul ^{[2
]}

机构：

[1] Abbott Labs, Global Pharmaceut Res & Dev, Abbott Pk, IL 60064 USA

[2] Abbott Boires Ctr, Dept Med Chem, Worcester, MA 01605 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 06期

关键词：

D O I：

10.1016/j.bmcl.2008.01.094

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 was designed based upon the structure of A-740003. Structure-activity relationship (SAR) studies focused on the piperazine moiety and the right hand side substitution. Compounds were assayed for activity at human and rat P2X7 receptors and compound 29 was found to possess potent activity (IC50 = 30-60 nM) at both species. (c) 2008 Elsevier Ltd. All rights reserved.

引用

页码：2093 / 2096

页数：4

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