In-silico Studies on Phthalimide GABA Analogs for Anticonvulsant Activity Against Sodium Channel and GABA-AT

Abstract

Introduction: GABA is a type of inhibitory neurotransmitter; it blocks or inhibits certain nerve transmission. Our nervous system is calmed by GABA, thus preventing excessive fear or anxiety is a simple and rapid approach to raise and maintain healthy mental health. Some medical conditions associated with a change in the level of GABA are anxiety and mood disorders, schizophrenia, autism spectrum disorder, depression, epilepsy, and seizures. The aim of this study to increase the activity of GABA which can be enhanced by the incorporation of anthracene, phthalimide, benzene, and thalidomide. Materials and methods: Insilico Docking study was carried out by using Auto Dock 4.0 against GABA-AT protein and the binding energy was found out to be -7.61kcal/mol. GABA-Phthalimide substitution, derivatives were designed as they possess a similar degree of anticonvulsant potency due to their phenytoin-like profile. The phthalimide pharmacophores interaction with voltage dependent sodium channels in neurons was investigated. Results and conclusion: This suggests the substitution of GABA as a possible lead compound. Therefore, in the present study, N, N-phthaloyl GABA combine with aniline a Noval compound 4-(1,3-dioxoisoindolin-2-yl)-N-phenylbutanamide is designed with improved anticonvulsant properties.