Synthesis, Anticonvulsant and Neurotoxicity Evaluation of Some Newer N-(2-benzoylbenzofuran-3-yl)-3-(substituted)-propanamide Analogs
Ashok K. Shakya,
Mohamed Jawed Ahsan,
A series of 12, N-(2-benzoylbenzofuran-3-yl)-3-(substituted)-propanamide analogs was designed and
synthesized to meet the pharmacophore requirement essential for anticonvulsant activity. All the compounds were
characterized by IR, 1H NMR and mass spectral data followed by their anticonvulsant evaluation according to the
Antiepileptic Drug Development Program (ADD) protocol. The present study has proved the hypothesis concerning the
pharmacophore model with essential binding sites. N-(2-benzoylbenzofuran-3-yl)-3-(4-(2-fluorophenyl)piperazin-1-yl)
propanamide, 6h was found to be the most active compound in both maximal electroshock seizure (MES) and
subcutaneous metrazol (scMET) seizure test at 30 and100 mg/kg respectively at 0.5 and 4.0 h.
Keywords: Amides, anticonvulsant agents, benzofuran, maximal electroshock seizure (MES), neurotoxicity, subcutaneous
metrazol (scMET) seizure.
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