Synthesis, Physicochemical and Anticonvulsant Properties of New N-4-arylpiperazin-1-yl Amides of (2-aza-1,3-dioxospiro [4.5] Dec-2-yl)-acetic Acid

As a continuation of our study on a number of 1,3-substituted pyrrolidine-2,5-diones, in this paper we report the synthesis, physicochemical and anticonvulsant properties of new derivatives of N-4-arylpiperazin-1-yl amides of (2-aza-1,3-dioxospiro[4.5]dec-2-yl)-acetic acid. The amides [II-X] were prepared by condensation of the formerly obtained (2-aza-1,3-dioxospiro[4.5]dec-2-yl)-acetic acid [I] with the appropriately substituted 4-arylpiperazines in DMF, in the presence of the N,N-carbonyldiimidazole (CDIM) reagent at room temperature. The compounds were tested for their anticonvulsant activity in the maximum electroshock seizure (MES) and the metrazole seizure threshold (sc. Met) tests. Some of them were active in the sc. Met test. The structures of the new amides were confirmed by their elemental and spectral analyses.