Abstract
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.
Central Nervous System Agents in Medicinal Chemistry
Title:Synthesis, Anticonvulsant and Neurotoxicity Evaluation of Some Newer N-(2-benzoylbenzofuran-3-yl)-3-(substituted)-propanamide Analogs
Volume: 13 Issue: 3
Author(s): Mehnaz Kamal, Ashok K. Shakya, Mohamed Jawed Ahsan and Talha Jawaid
Affiliation:
Keywords: Amides, anticonvulsant agents, benzofuran, maximal electroshock seizure (MES), neurotoxicity, subcutaneous metrazol (scMET) seizure.
Abstract: 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.
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Cite this article as:
Kamal Mehnaz, Shakya K. Ashok, Ahsan Jawed Mohamed and Jawaid Talha, Synthesis, Anticonvulsant and Neurotoxicity Evaluation of Some Newer N-(2-benzoylbenzofuran-3-yl)-3-(substituted)-propanamide Analogs, Central Nervous System Agents in Medicinal Chemistry 2013; 13 (3) . https://dx.doi.org/10.2174/1871524913666131122160828
DOI https://dx.doi.org/10.2174/1871524913666131122160828 |
Print ISSN 1871-5249 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6166 |
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