Synthesis and in vivo evaluation of bicyclic gababutins

被引：32

作者：

Blakemore, David C. ^{[1
]}

Bryans, Justin S. ^{[1
]}

Carnell, Pauline ^{[1
]}

Carr, Christopher L. ^{[1
]}

Chessum, Nicola E. A. ^{[1
]}

Field, Mark J. ^{[1
]}

Kinsella, Natasha ^{[1
]}

Osborne, Simon A. ^{[1
]}

Warren, Andrew N. ^{[1
]}

Williams, Sophie C. ^{[1
]}

机构：

[1] Pfizer Ltd, Global Res & Dev, Sandwich Labs, Sandwich CT13 9NJ, Kent, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 02期

关键词：

Gabapentin; Gababutin; Pregabalin; Pain; NEUROPATHIC PAIN; CALCIUM-CHANNEL; PREGABALIN; GABAPENTIN; LIGANDS; ANALOGS;

D O I：

10.1016/j.bmcl.2009.11.118

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Synthesis of a number of bicyclic five-membered ring derivatives of gabapentin led to the identification of two compounds, (-)-(11A) and (20A) which both had an excellent level of potency against alpha(2)delta and were pro. led in an in vivo model of neuropathic pain. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：461 / 464

页数：4

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