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
-
Juvenile Neuronal Ceroid-Lipofuscinosis (Batten Disease): A Brief Review and Update
Current Molecular Medicine SIRT1 Promotes Neuronal Fortification in Neurodegenerative Diseases through Attenuation of Pathological Hallmarks and Enhancement of Cellular Lifespan
Current Neuropharmacology History and Therapeutic Use of MAO-A Inhibitors: A Historical Perspective of MAO-A Inhibitors As Antidepressant Drug
Current Topics in Medicinal Chemistry Coenzyme Q10 and Neurological Diseases: An Update
Letters in Drug Design & Discovery From Anreps Phenomenon to Myocardial Hypertrophy: Role of the Na+/H+ Exchanger
Current Cardiology Reviews Subject Index To Volume 12
Current Pharmaceutical Design Epidemiology of Major Congenital Malformations with Specific Focus on Teratogens
Current Drug Safety Anxiety: A Systematic Review of Neurobiology, Traditional Pharmaceuticals and Novel Alternatives from Medicinal Plants
CNS & Neurological Disorders - Drug Targets Astrocyte-Neuron Interaction at Tripartite Synapses
Current Drug Targets The Sustained Effects on Tear Volume of Pilocarpine Hydrochloride in Gelatin by Hydrogel Administered by An Implant-mediated Drug Delivery System
Current Drug Delivery Engineered Probiotic and Prebiotic Nutraceutical Supplementations in Combating Non-communicable Disorders: A Review
Current Pharmaceutical Biotechnology Neurological Aspects of Medical Use of Cannabidiol
CNS & Neurological Disorders - Drug Targets Non-Selective Cation Channel Blockers: Potential Use in Nervous System Basic Research and Therapeutics
Mini-Reviews in Medicinal Chemistry Huntingtons Disease: The Value of Transcranial Meganetic Stimulation
Current Medicinal Chemistry Understanding the Molecular Mechanisms of Betel miRNAs on Human Health
MicroRNA Cooling the Injured Brain: How Does Moderate Hypothermia Influence the Pathophysiology of Traumatic Brain Injury
Current Pharmaceutical Design Quinoline Derivatives: Candidate Drugs for a Class B G-Protein Coupled Receptor, the Calcitonin Gene-Related Peptide Receptor, a Cause of Migraines
CNS & Neurological Disorders - Drug Targets Clinical Profile of Mortality among Chronic Schizophrenic Patients: A Local Pilot Survey in Iran
Current Psychiatry Research and Reviews Preparation and Development of Oral Controlled Release w/o/w Multiple Emulsion of Carbamazepine
Drug Delivery Letters ATP-Sensitive Potassium Channels
Current Pharmaceutical Design