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RESEARCH ARTICLE
Year : 2017  |  Volume : 6  |  Issue : 1  |  Page : 13-22

Isatin-based anticonvulsant agents: Synthesis and antiseizure evaluation in mice


1 Pharmaceutical Sciences Research Center, School of Pharmacy, Kermanshah University of Medical Sciences, Kermanshah; Isfahan Pharmaceutical Sciences Research Center, Isfahan; Department of Medicinal Chemistry, Faculty of Pharmacy, Kermanshah University of Medical Sciences, Kermanshah, Iran
2 Pharmaceutical Sciences Research Center, School of Pharmacy, Kermanshah University of Medical Sciences; Department of Pharmacology, Toxicology and Medical Services, Faculty of Pharmacy, Kermanshah University of Medical Sciences, Kermanshah, Iran
3 Department of Medicinal Chemistry, Faculty of Pharmacy, Kermanshah University of Medical Sciences; Students Research Committee, Kermanshah University of Medical Sciences, Kermanshah, Iran
4 Pharmaceutical Sciences Research Center, School of Pharmacy, Kermanshah University of Medical Sciences; Department of Medicinal Chemistry, Faculty of Pharmacy, Kermanshah University of Medical Sciences, Kermanshah, Iran

Correspondence Address:
Alireza Aliabadi
Pharmaceutical Sciences Research Center, School of Pharmacy, Kermanshah University of Medical Sciences; Department of Medicinal Chemistry, Faculty of Pharmacy, Kermanshah University of Medical Sciences, Kermanshah
Iran
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Source of Support: None, Conflict of Interest: None


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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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