Carboxylate bioisosteres of gabapentin.

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 α 2 -δ protein. Further characterization of α 2 -δ binding compounds 14a and 14b revealed a similar pattern of functional in vitro and in vivo activity to gabapentin 1 .