Synthesis and biological evaluation of new derivatives of 2-substituted 4-hydroxybutanamides as GABA uptake inhibitors

► Synthesis of N-arylalkyl-2-(4-diphenylmethylpiperazin-1-yl)-4-hydroxybutyramide. ► Activity of murine GABA transport proteins GAT1-GAT4. ► The most active inhibitor with pKi = 4.96 in GAT1-binding assay.