Carboxylate bioisosteres of pregabalin

Abstract Several β-amino tetrazole analogs of gabapentin 1 and pregabalin 2 were prepared by one of two convergent, highly efficient routes, and their affinity for the α 2 –δ protein examined. Two select compounds with potent affinity for α 2 –δ, 8a and 16a , were subsequently tested in vivo in an audiogenic seizure model and found to elicit protective effects.