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
-
Discovery of Substituted N-(6-Chloro-3-cyano-4-phenyl-4H-chromen-2-yl)- 2-(4-chloro-phenoxy)-acetamide for Biphasic Anticancer and Anticonvulsant Activities
Medicinal Chemistry Genetic Studies on the Role of T-Type Ca2+ Channels in Sleep and Absence Epilepsy
CNS & Neurological Disorders - Drug Targets Brain Serotonin, Psychoactive Drugs, and Effects on Reproduction
Central Nervous System Agents in Medicinal Chemistry Impaired Functional Connectivity of the Thalamus in Alzheimer’ s Disease and Mild Cognitive Impairment: A Resting-State fMRI Study
Current Alzheimer Research Design, Synthesis, and Screening of Hybrid Benzothiazolyl-Oxadiazoles as Anticonvulsant Agents
Letters in Drug Design & Discovery Bis-dihydroisoxazolines: Synthesis, Structural Elucidation, Antimicrobial Evaluation, and DNA Photocleavage Assay
Current Organic Synthesis Calcium Channel α2δ Subunits: Structure, Functions and Target Site for Drugs
Current Neuropharmacology Ontologies of Drug Discovery and Design for Neurology, Cardiology and Oncology
Current Pharmaceutical Design Preface
Current Pharmaceutical Design Nicotinic Receptors in Neurodegeneration
Current Neuropharmacology The Role of Neuropeptides and Neurohormones in Neurogenic Cardiac Arrhythmias
Current Drug Targets - Cardiovascular & Hematological Disorders Editorial [Hot Topic: Functions and Metabolism of Brain Nucleosides and their Metabolites (Guest Editors: Zsolt Kovacs & Arpad Dobolyi)]
Current Topics in Medicinal Chemistry Antiepileptics and the Treatment of Neuropathic Pain: Evidence from Animal Models
Current Pharmaceutical Design Editorial (Thematic Issue: Global Trends in Nanotechnological Approaches for Various Health Issues – Volume II)
Current Drug Metabolism Neuroprotective Effects of Low-dose Lithium in Individuals at Ultra-high Risk for Psychosis. A Longitudinal MRI/MRS Study
Current Pharmaceutical Design Comparison of Status Epilepticus Models Induced by Pilocarpine and Nerve Agents - A Systematic Review of the Underlying Aetiology and Adopted Therapeutic Approaches
Current Medicinal Chemistry Characterisation of a Neural Teratogenicity Assay Based on Human ESCs Differentiation Following Exposure to Valproic Acid
Current Medicinal Chemistry Effect of Levetiracetam on Cognitive Function and Clonic Seizure Frequency in Children with Epilepsy
Current Molecular Medicine Seizures and Sodium Hydrogen Exchangers: Potential of Sodium Hydrogen Exchanger Inhibitors as Novel Anticonvulsants
CNS & Neurological Disorders - Drug Targets Persons with Co-Existing Neurological Disorders: Risk Analysis, Considerations and Management in COVID-19 Pandemic
CNS & Neurological Disorders - Drug Targets