Carboxylate bioisosteres of gabapentin

被引：19

作者：

Burgos-Lepley, CE

Thompson, LR

Kneen, CO

Osborne, SA

Bryans, JS

Capiris, T

Suman-Chauhan, N

Dooley, DJ

Donovan, CM

Field, MJ

Vartanian, MG

Kinsora, JJ

Lotarski, SM

El-Kattan, A

Walters, K

Cherukury, M

Taylor, CP

Wustrow, DJ

Schwarz, JB

机构：

[1] Michigan Labs, Pfizer Global Res & Dev, Ann Arbor, MI 48105 USA

[2] Sandwich Labs, Sandwich CT13 9NJ, Kent, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 09期

关键词：

gabapentin; alpha(2)-delta subunit;

D O I：

10.1016/j.bmcl.2005.05.016

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of carboxylate bioisosteres of structures related to gabapentin 1 have been prepared. When the carboxylate was replaced by a tetrazole, this group was recognized by the alpha(2)-delta protein. Further characterization Of alpha(2)-delta binding compounds 14a and 14b revealed a similar pattern of functional in vitro and in vivo activity to gabapentin 1. (C) 2005 Elsevier Ltd. All rights reserved.

引用

收藏

页码：2333 / 2336

页数：4

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