Abstract

REVIEW ON ANTICONVULSANT EVALUATION OF SOME NEWER BENZIMIDAZOLEDERIVATIVES: DESIGN AND SYNTHESIS

Palmate Ankita L.*, Bavge S. B., Patel A. C. and Ingle P. V.

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Abstract

A series of new 2-[(1-substituted phenylethylidine) hydrazine]-N-phenyl-1H-benzo[d]imidazole-1-carbothioamides (4a-n) were designed and synthesized to have the pharmacophoric elements essential for anti-convulsant activity. The key step in the synthesis of the title compounds involves the reaction of 2-mercapto-benzimidazole with hydrazine hydrate, substituted acetophenones and phenylisothiocyanate to get the com-pounds in good yields. All the newly synthesized compounds were screened by two most adopted models, max-imal electroshock seizure (MES) and subcutaneous pentylenetetrazole (scPTZ). Interestingly, compounds 4e, 4f, 4g, 4h and 4j exhibited potent anticonvulsant results and in the neurotoxicity screening, most of the com-pounds were devoid of toxicity at the dose of 60 and 100 mg/kg.

Keywords: 2 mercaptobenzimdiazole, Maximal elctroahock seziure test, Subcutaneous pentylenetetrazole, Anticonvulsant activity, Neurotoxcitiy.