Literature DB >> 15946842

Carboxylate bioisosteres of gabapentin.

Carmen E Burgos-Lepley1, 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, Ayman El-Kattan, Karen Walters, Madhu Cherukury, Charles P Taylor, David J Wustrow, Jacob B Schwarz.   

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 alpha2-delta protein. Further characterization of alpha2-delta binding compounds 14a and 14b revealed a similar pattern of functional in vitro and in vivo activity to gabapentin 1.

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Year:  2005        PMID: 15946842     DOI: 10.1016/j.bmcl.2005.05.016

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  1 in total

1.  An efficient synthesis of gamma-amino acids and attempts to drive its enantioselectivity.

Authors:  Salvador Gil; Margarita Parra; Pablo Rodríguez
Journal:  Molecules       Date:  2008-03-27       Impact factor: 4.411

  1 in total

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