Design and synthesis of novel 2-(5-(4-aryl)-4,5-dihydro-1H-pyrazol-3-yl)-1-(substituted aminomethyl)-1H-benzimidazole as potent anticonvulsants
A variety of novel 2-(5-(4-aryl)-4,5-dihydro-1H-pyrazol-3-yl)-1-(substitutedaminomethyl)-1H-benzimidazole 5a–5l have been synthesized from o-phenylenediamine by a multi-step synthesis. Antiepileptic screening of the title compounds was performed using maximal electroshock and subcutaneous pentylenetetrazole seizures tests while the neurotoxicity was determined by rotorod test. In the preliminary screening, compounds 5d, 5e, 5f and 5l were found active in maximal electroshock model; while 5d, 5e, 5f and 5k showed significant antiepileptic activity in subcutaneous pentylenetetrazole seizure model. Further all these five compounds were administered to rats at 30 mg/kg dose in oral route and found that compounds 5e and 5f showed better activity than Phenytoin. These compounds 5e and 5f revealed protection in maximal electroshock after intraperitoneal administration at a dose of 30 mg/kg (0.5 h and 4.0 h). These compounds also provided protection in the subcutaneous pentylenetetrazole seizure at a dose of 100 mg/kg (0.5 h) and 300 mg/kg (4 h).
KeywordsBenzimidazole Pyrazole Epilepsy In vivo studies Neurotoxicity
The authors gratefully acknowledge the Pfizer limited and GITAM University for providing infrastructure facilities to carry out this research work.
Compliance with ethical standards
Conflict of interests
The authors declares that they have no competing interests.
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