ISSN : 0975-9492


Open Access

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Title : Synthesis, Characterization And Evaluation Of 2-Imino Benzothiazole Derivatives As Anticonvulsant Agents
Authors : Ranjana Singh, Suruchi Sharma
Keywords : Benzothiazole, Schiff base, anticonvulsant, neurotoxicity, max. electroshock seizure (MES).
Issue Date : May 2014
Abstract :
Purpose - To synthesize potent bentothiazole derivatives screened to possess anti-convulsant activity as a way forward for treatment of epilepsy.
Method: The present work emphasizes on synthesis of new series of 2-amino-6-substituted benzothiazole (A-D) by using 4-substituted aniline and potassium thiocyanate in presence of bromine in glacial acetic acid which further treated with various substituted aromatic aldehydes in presence of glacial acetic acid to get the 2-imino-benzothiazole derivatives (2A to 2I). (6-Substituted-benzothiazol-2-yl)-(4-substituted-benzylidene)-amine derivatives obtained from the reactional sequence were injected intraperitoneally into mice and evaluated by the maximal electroshock (MES), neurotoxicity screen using rotarod at the dose of 30 mg/kg. Phenytoin was used as the standard for the comparison at the dose level of 25 mg/kg.
Results: The MES activity indicated significant anticonvulsant activity for all of the test compounds. However, they were found to be less potent when compared with the reference standard Phenytoin. Within the series A, B, C and D compounds of series B with substitution of -F at 6th position of benzothiazole showed maximum potency.
Conclusion: All the compounds showed protections against seizures in the range 50-75% indicative of the promising nature of the compounds against seizure spread. Thus it can be concluded that substitution of 6th-position with fluoro, chloro, bromo and nitro groups (A-D) at the terminal benzothiazole ring is beneficial for anticonvulsant activity.
Page(s) : 213-217
ISSN : 0975-9492
Source : Vol. 5, No.5