Synthesis, Anticonvulsant and Neurotoxicity Evaluation of Some Newer N-(2-benzoylbenzofuran-3-yl)-3-(substituted)-propanamide Analogs

Author(s): Mehnaz Kamal, Ashok K. Shakya, Mohamed Jawed Ahsan, Talha Jawaid

Journal Name: Central Nervous System Agents in Medicinal Chemistry
Formerly Current Medicinal Chemistry - Central Nervous System Agents

Volume 13 , Issue 3 , 2013

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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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Article Details

Year: 2013
Published on: 22 November, 2013
Page: [159 - 165]
Pages: 7
DOI: 10.2174/1871524913666131122160828
Price: $65

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