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Neuropathic pain is characterized by a neuronal hyperexcitability in damaged areas of the peripheral or central nervous system. The neuronal hyperexcitability in neuropathic pain have many common features with the cellular changes in epilepsy. This has led to the use of anticonvulsant drugs for the treatment of neuropathic pain. The present study aims at design and synthesis of two types of γ-aminobutyric acid (GABA) derivatives incorporated in the 1, 2, 4-triazol-2H-one nucleus and their evaluation for antiepileptic, peripheral analgesic, antiallodynic and antihyperalgesic potential in neuropathic pain models. Most of the synthesized triazole derivatives of GABA produced antiepileptic, antinocciceptive, antihyperalgesic, and antiallodynic actions and hence emerges as a promising lead for new drug development for the treatment of epilepsy and neuropathic pain.

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.