Abstract
A series of 2-(substituted benzylidene)-7-(4-fluorophenyl)-5-(furan-2-yl)-2H-thiazolo[3,2-a]pyrimidin-3(7H)- one derivatives were newly synthesized by the reaction of 7-(4-fluoro phenyl)-5-(furan-2-yl)-2H-thiazolo[3,2- a]pyrimidin-3(7H)-one (3) with appropriate substituted benzaldehyde in the presence of anhydrous sodium acetate and glacial acetic acid. Their structures were confirmed by IR, 1H NMR, mass and elemental analyses. These novel thiazolopyrimidine derivatives were screened for their antiepileptic activity by using MES: Maximal Electroshock Seizure test and ScPTZ: Subcutaneous pentylenetetrazole seizures tests. The neurotoxicity was determined by rotorod test. Among these compounds 4f revealed protection in MES at a dose of 30 mg kg-1 and 100 mg kg-1 0.5 h and 4 h after i.p. administration respectively. This molecule provided also protection in the scPTZ at a dose of 300 mg kg-1 in both time intervals.
Letters in Drug Design & Discovery
Title:Antiepileptic Activity of Novel 2-(substituted benzylidene)-7-(4- fluorophenyl)-5-(furan-2-yl)-2H-thiazolo[3,2-a]pyrimidin-3(7H)-one Derivatives
Volume: 10 Issue: 3
Author(s): T. Panneer Selvam, V. Karthick, P. Vijayaraj Kumar and M. Ashraf Ali
Affiliation:
Keywords: Thiazolopyrimidine; Antiepilepsy; Neurotoxicity.
Abstract: A series of 2-(substituted benzylidene)-7-(4-fluorophenyl)-5-(furan-2-yl)-2H-thiazolo[3,2-a]pyrimidin-3(7H)- one derivatives were newly synthesized by the reaction of 7-(4-fluoro phenyl)-5-(furan-2-yl)-2H-thiazolo[3,2- a]pyrimidin-3(7H)-one (3) with appropriate substituted benzaldehyde in the presence of anhydrous sodium acetate and glacial acetic acid. Their structures were confirmed by IR, 1H NMR, mass and elemental analyses. These novel thiazolopyrimidine derivatives were screened for their antiepileptic activity by using MES: Maximal Electroshock Seizure test and ScPTZ: Subcutaneous pentylenetetrazole seizures tests. The neurotoxicity was determined by rotorod test. Among these compounds 4f revealed protection in MES at a dose of 30 mg kg-1 and 100 mg kg-1 0.5 h and 4 h after i.p. administration respectively. This molecule provided also protection in the scPTZ at a dose of 300 mg kg-1 in both time intervals.
Export Options
About this article
Cite this article as:
Panneer Selvam T., Karthick V., Vijayaraj Kumar P. and Ashraf Ali M., Antiepileptic Activity of Novel 2-(substituted benzylidene)-7-(4- fluorophenyl)-5-(furan-2-yl)-2H-thiazolo[3,2-a]pyrimidin-3(7H)-one Derivatives, Letters in Drug Design & Discovery 2013; 10 (3) . https://dx.doi.org/10.2174/1570180811310030003
DOI https://dx.doi.org/10.2174/1570180811310030003 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
- 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
Related Articles
-
Synthesis and Evaluation of Novel Diazaspiro Hydantoins as Potential Anticonvulsants
Central Nervous System Agents in Medicinal Chemistry Activity-Dependent Release of Adenosine: A Critical Re-Evaluation of Mechanism
Current Neuropharmacology Green Tea, A Medicinal Food with Promising Neurological Benefits
Current Neuropharmacology Angiotensin Mediated Oxidative Stress and Neuroprotective Potential of Antioxidants and AT1 Receptor Blockers
Mini-Reviews in Medicinal Chemistry Ion Channels and Epilepsy
Current Pharmaceutical Design Maternal Choline Supplementation: A Potential Prenatal Treatment for Down Syndrome and Alzheimer’s Disease
Current Alzheimer Research Pharmacology of Voltage-Gated Proton Channels
Current Pharmaceutical Design Triggers of Cell Death in the Developing Brain
Current Pediatric Reviews Nitric Oxide, Peroxynitrite, Peroxynitrous Acid, Nitroxyl, Nitrogen Dioxide, Nitrous Oxide: Biochemical Mechanisms and Bioaction
Current Bioactive Compounds Editorial (Thematic Issue: Global Trends for Nanotechnological Approaches in Various Health Issues - Part 1)
Current Drug Metabolism The Potential of Pregabalin in Neurology, Psychiatry and Addiction: A Qualitative Overview
Current Pharmaceutical Design Melatonin, its Metabolites and its Synthetic Analogs as Multi-Faceted Compounds: Antioxidant, Prooxidant and Inhibitor of Bioactivation Reactions
Current Medicinal Chemistry In-vitro Antioxidant activity of ‘Aswathy Chooranam’- a Siddha Drug
Current Traditional Medicine Dynamic Expression of MicroRNAs (183, 135a, 125b, 128, 30c and 27a) in the Rat Pilocarpine Model and Temporal Lobe Epilepsy Patients
CNS & Neurological Disorders - Drug Targets Machine Learning, Molecular Modeling, and QSAR Studies on Natural Products Against Alzheimer’s Disease
Current Medicinal Chemistry Editorial (Thematic Issue: Global Trends in Nanotechnological Approaches for Various Health Issues – Volume II)
Current Drug Metabolism Cyclooxygenase and Neuroinflammation in Parkinsons Disease Neurodegeneration
Current Neuropharmacology Novel Therapeutic Strategies for Dementia
CNS & Neurological Disorders - Drug Targets Pediatric Catatonia: Updating An Old Syndrome in Young People
Current Psychiatry Reviews Drug Therapy for Patients with Eating Disorders
Current Drug Targets - CNS & Neurological Disorders