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.
Export Options
About this article
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 |
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements
Related Articles
-
Green Tea, A Medicinal Food with Promising Neurological Benefits
Current Neuropharmacology Drug Repositioning for Treatment of Movement Disorders: From Serendipity to Rational Discovery Strategies
Current Topics in Medicinal Chemistry Winning a Won Game: Caffeine Panacea for Obesity Syndemic
Current Neuropharmacology Editorial [Hot Topic: PET and SPECT in Drug Evaluation and Drug Design Imaging Inflammatory Processes, Tumors, and the Endocannabinoid System(Executive Editor: Aren van Waarde)]
Current Pharmaceutical Design Patent Selections:
Recent Patents and Topics on Imaging (Discontinued) The Prophylactic Use of Antiepileptic Drugs in Patients Scheduled for Neurosurgery
Current Pharmaceutical Design Nutraceuticals, A New Challenge for Medicinal Chemistry
Current Medicinal Chemistry GABA Receptors: Pharmacological Potential and Pitfalls
Current Pharmaceutical Design Cannabinoids and Sensory Neurones
Current Neuropharmacology Substance P Regulation in Epilepsy
Current Neuropharmacology Structurally Unprecedented Metabolites from Marine Sponges
Current Organic Chemistry Histone Deacetylase Inhibitors: Therapeutic Agents and Research Tools for Deciphering Motor Neuron Diseases
Current Medicinal Chemistry Subject Index To Volume 5
CNS & Neurological Disorders - Drug Targets Alkaloids Pharmacological Activities - Prospects for the Development of Phytopharmaceuticals for Neurodegenerative Diseases
Current Pharmaceutical Biotechnology Cellular and Network Mechanisms Underlying Memory Impairment Induced by Amyloid β Protein
Protein & Peptide Letters Cognitive Improvement by Photic Stimulation in a Mouse Model of Alzheimer’s Disease
Current Alzheimer Research N-acetylcysteine Versus Placebo for Treating Nail Biting, a Double Blind Randomized Placebo Controlled Clinical Trial
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Dry Age-Related Macular Degeneration: Recent Progress of Therapeutic approaches
Current Molecular Pharmacology Infectious Agents and Neurodegenerative Diseases: Exploring the Links
Current Topics in Medicinal Chemistry A New Interpretative Paradigm for Conformational Protein Diseases
Current Protein & Peptide Science