Abstract
DESIGN AND SYNTHESIS OF NOVEL SUBSTITUTED BENZIMIDAZOLE ANALOGS AS POTENT ANTICONVULSANT AGENTS

Krishna Veni Chikkula and Raja S.*

ABSTRACT

Based on pharmacophore model requirement a series of novel heterocyclic substituted benzimidazole derivatives were synthesized as potent anticonvulsant agents. The synthesized compounds were characterized by FT-IR, 1H-NMR, Mass spectroscopy and bases of elemental analysis. MES test and scPTZ test were performed for screening anticonvulsant activity. Moreover all potent compounds were examined for its neurotoxicity by rota rod test. Results revealed that entire series of compounds exhibited mild to good anticonvulsant activity. In general it was found that the pyrazolone derivatives Va-Vi exhibited higher antiepileptic activity than the isoxazolone derivatives III and pyridimidinone derivatives IVa-IVb. Among all test compounds the most active compound was 4-(2-(4-(1H-benzimidazol-2-yl)phenyl)hydrazono)-1-(4-methoxyphenyl)-3-amino-1H-pyrazol-5(4H)-one Ve and the least active was 4-(2-(4-(1H-benzimidazol-2-yl)phenyl)hydrazono)-3-aminoisoxazol-5(4H)-one III.

Keywords: Benzimidazole, Isoxazole, Pyrimidine, Pyrazole, MES test, scPTZ test.


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