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

ISSN: 1875-6166 (Online)
ISSN: 1871-5249 (Print)


Volume 14, 2 Issues, 2014


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Central Nervous System Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Cancer Agents

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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 and Talha Jawaid

Affiliation: Faculty of Pharmacy, Integral University, Dasauli, Kursi Road, Lucknow, Uttar Pradesh 226 026, India.

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.

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Article Details

Volume: 13
Issue Number: 3
First Page: 159
Last Page: 165
Page Count: 7
DOI: 10.2174/1871524913666131122160828
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