Novel and potent 3-(2,3-dichlorophenyl)-4-(benzyl)-4H-1,2,4-triazole P2X7 antagonists

被引：42
作者：
Carroll, William A.
Kalvin, Douglas M.
Medranoa, Arturo Perez
Florjancic, Alan S.
Wang, Ying
Donnelly-Roberts, Diana L.
Namovic, Marian T.
Grayson, George
Honore, Prisca
Jarvis, Michael F.
机构：
[1] Abbott Labs, Neurosci Res, Abbott Pk, IL 60064 USA
[2] Abbott Labs, Med Chem Technol, Abbott Pk, IL 60064 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 14期
关键词：
P2X(7) antagonist; neuropathic pain;
D O I：
10.1016/j.bmcl.2007.04.075
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Structure-activity relationship (SAR) studies were conducted around early tetrazole-based leads 3 and 4. Replacements for the tetrazole core were investigated and the pendant benzyl substitution was reoptimized with a triazole isostere. Triazole-based P2X(7) antagonists were identified with similar potency to the lead compound 4 but with improved physiochemical properties. Compound 12 was active in a rat model of neuropathic pain. (C) 2007 Elsevier Ltd. All rights reserved.
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收藏
页码：4044 / 4048
页数：5
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