Design and synthesis of anticonvulsants from a combined phthalimide–GABA–anilide and hydrazone pharmacophore

Two series of pharmacophoric hybrids of phthalimide–GABA–anilides/hydrazones were designed and synthesized and evaluated for their anticonvulsant and neurotoxic properties. The structures of the synthesized compounds were confirmed by the use of their spectral data besides elemental analysis. Initial anticonvulsant screening was performed using intraperitoneal (i.p.) maximal electroshock-induced seizure (MES), subcutaneous pentylenetetrazole (scPTZ), subcutaneous strychnine (scSTY), and intraperitoneal picrotoxin (ipPIC)-induced seizure threshold tests. All of the compounds were ineffective in the MES test. Most of the compounds were found to be effective in the scSTY and ipPIC models and very few compounds showed protection in the scPTZ model.

Two series of N,N-phthaloyl GABA derivatives were synthesized as amides and acid hydrazones and evaluated for their anticonvulsant and neurotoxic properties. Most of the compounds were found to be effective in the scSTY and ipPIC models and very few compounds showed protection in the scPTZ model.Figure optionsDownload as PowerPoint slide