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ID: ALA1146981

Journal: Bioorg Med Chem Lett

Title: Carboxylate bioisosteres of gabapentin.

Authors: 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.

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.

CiteXplore: 15946842

DOI: 10.1016/j.bmcl.2005.05.016