Abstract
Based on the positive background of CNS activity of isatin analogs, a new series of isatin-based anticonvulsant derivatives (3a-3m) were designed and synthesized. According to the pharmacophoric necessities of anticonvulsant three essential parts namely aromatic ring (AR), electron donor (ED) group and hydrogen bond acceptor/donor (HAD) group were considered in the structure of designed compounds (3a-3m). Isatin was treated with various derivatives of aniline in the presences of glacial acetic acid under reflux condition. Two standard convulsive protocols namely maximal electroshock (MES) and pentylenetetrazole (PTZ) were utilized to investigate the anticonvulsant efficacy of these series. Besides, rotorod test was used to assess the neurotoxicity of corresponding compounds. Fortunately, the most of tested derivatives exhibited remarkable preventive effect in both applied convulsive models with low incidence of neurotoxicity in rotorod test.
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Copyright
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