Synthesis and SAR development of novel P2X7 receptor antagonists for the treatment of pain: Part 2

被引：12

作者：

Brumfield, Stephanie ^{[1
]}

Matasi, Julius J. ^{[1
]}

Tulshian, Deen ^{[1
]}

Czarniecki, Michael ^{[1
]}

Greenlee, William ^{[1
]}

Garlisi, Charles ^{[1
]}

Qiu, Hongchen ^{[1
]}

Devito, Kristine ^{[1
]}

Chen, Shu-Cheng ^{[1
]}

Sun, Yongliang ^{[1
]}

Bertorelli, Rosalia ^{[1
]}

Ansell, Justin ^{[1
]}

Geiss, William ^{[2
]}

Van-Duc Le ^{[2
]}

Martin, Gregory S. ^{[2
]}

Vellekoop, Samuel A. ^{[2
]}

Haber, James ^{[2
]}

Allard, Melissa L. ^{[2
]}

机构：

[1] Merck Res Labs, Kenilworth, NJ 07033 USA

[2] Albany Mol Res Inc, Albany, NY 12212 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2011年 / 21卷 / 24期

关键词：

P2X(7); Purine derivatives; Inflammatory pain; Neuropathic pain; MODEL; RAT;

D O I：

10.1016/j.bmcl.2011.10.037

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Novel P2X(7) antagonists were developed using a purine scaffold. These compounds were potent and selective at the P2X(7) receptor in human and rodent as well as efficacious in rodent pain models. Compound 15a was identified to have oral potency in several pain models in rodent similar to naproxen, gabapentin and pregabalin. Structure-activity relationship (SAR) development and results of pain models are presented. (C) 2011 Elsevier Ltd. All rights reserved.

引用

页码：7287 / 7290

页数：4

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