| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1374696 | Bioorganic & Medicinal Chemistry Letters | 2006 | 4 Pages |
Abstract
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 α2-δ protein. Further characterization of α2-δ binding compounds 14a and 14b revealed a similar pattern of functional in vitro and in vivo activity to gabapentin 1.
Graphical abstractRing expansion and acid replacement with tetrazole furnished a compound with a similar pattern of activity to gabapentin.Figure optionsDownload full-size imageDownload as PowerPoint slide
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Carmen E. Burgos-Lepley, Lisa R. Thompson, Clare O. Kneen, Simon A. Osborne, Justin S. Bryans, Thomas Capiris, Nirmala Suman-Chauhan, David J. Dooley, Cindy M. Donovan, Mark J. Field, Mark G. Vartanian, Jack J. Kinsora, Susan M. Lotarski,