Abstract
Novel N3 aryl/heteroaryl substituted 2-((benzyloxy and phenylthio) methyl) 6,7-dimethoxyquinazolin-4(3H)- ones (8a-8l) were synthesized and evaluated for their anticonvulsant activity using various models of epilepsy, such as maximal electroshock (MES), subcutaneous pentylenetetrazole (scPTZ) and intracerebroventricular AMPA (α-amino-3- hydroxy-5-methyl-4-isoxazolepropionic acid)-induced seizures in mice. The rotarod test has been used to determine the acute neurotoxicity. Further, the serum enzymatic activities of aspartate aminotransferase (AST) and alanine aminotransferase (ALT) were assessed along with histopathological examination of liver. Among all the derivatives, compound 8f displayed significant activity profile based on the overall magnitude of activity and minimum neurotoxicity.
Keywords: Anticonvulsant activity, AMPA induced seizure, hepatotoxicity, neurotoxicity, quinazolin-4(3H)-ones, synthesis.
Medicinal Chemistry
Title:Design, Synthesis and Pharmacological Evaluation of N3 Aryl/ Heteroaryl Substituted 2-((Benzyloxy and Phenylthio) Methyl) 6,7- dimethoxyquinazolin-4(3H)-ones as Potential Anticonvulsant Agents
Volume: 10 Issue: 8
Author(s): Nirupam Das, Anupam G. Banerjee and Sushant K. Shrivastava
Affiliation:
Keywords: Anticonvulsant activity, AMPA induced seizure, hepatotoxicity, neurotoxicity, quinazolin-4(3H)-ones, synthesis.
Abstract: Novel N3 aryl/heteroaryl substituted 2-((benzyloxy and phenylthio) methyl) 6,7-dimethoxyquinazolin-4(3H)- ones (8a-8l) were synthesized and evaluated for their anticonvulsant activity using various models of epilepsy, such as maximal electroshock (MES), subcutaneous pentylenetetrazole (scPTZ) and intracerebroventricular AMPA (α-amino-3- hydroxy-5-methyl-4-isoxazolepropionic acid)-induced seizures in mice. The rotarod test has been used to determine the acute neurotoxicity. Further, the serum enzymatic activities of aspartate aminotransferase (AST) and alanine aminotransferase (ALT) were assessed along with histopathological examination of liver. Among all the derivatives, compound 8f displayed significant activity profile based on the overall magnitude of activity and minimum neurotoxicity.
Export Options
About this article
Cite this article as:
Das Nirupam, Banerjee G. Anupam and Shrivastava K. Sushant, Design, Synthesis and Pharmacological Evaluation of N3 Aryl/ Heteroaryl Substituted 2-((Benzyloxy and Phenylthio) Methyl) 6,7- dimethoxyquinazolin-4(3H)-ones as Potential Anticonvulsant Agents, Medicinal Chemistry 2014; 10 (8) . https://dx.doi.org/10.2174/1573406410666140402152044
DOI https://dx.doi.org/10.2174/1573406410666140402152044 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
![](/images/wayfinder.jpg)
- 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 Anticonvulsant Activity of 3-(alkylamino, alkoxy)-1,3,4,5- Tetrahydro-2H-benzo [b] azepine-2-one Derivatives
CNS & Neurological Disorders - Drug Targets Machine Learning Approaches for Cognitive State Classification and Brain Activity Prediction: A Survey
Current Bioinformatics Treatment of Central Nervous System Tuberculosis Infections and Neurological Complications of Tuberculosis Treatment
Current Pharmaceutical Design Structure-Activity Studies on Alpha-Conotoxins
Current Pharmaceutical Design Pyrrole: Chemical Synthesis, Microwave Assisted Synthesis, Reactions and Applications: A Review
Current Organic Chemistry An Update on Overcoming MDR1-Mediated Multidrug Resistance in Cancer Chemotherapy
Current Pharmaceutical Design Bridging Over the Troubled Heterogeneity of SPG-Related Pathologies: Mechanisms Unite What Genetics Divide
Current Molecular Medicine Naturally Occurring and Related Synthetic Cannabinoids and their Potential Therapeutic Applications
Recent Patents on CNS Drug Discovery (Discontinued) Chvostek's Sign in Paediatric Practice
Current Pediatric Reviews Mathematical Modelling and Feature Extraction for Probing Crucial Changes Associated with Alzheimers Disease
Current Medical Imaging Chinese Herbal Medicine Interventions in Neurological Disorder Therapeutics by Regulating Glutamate Signaling
Current Neuropharmacology In Vitro Modeling of the Blood-Brain Barrier: Simplicity Versus Complexity
Current Pharmaceutical Design Defining the Mechanism of Action of 4-Phenylbutyrate to Develop a Small-Molecule-Based Therapy for Alzheimers Disease
Current Medicinal Chemistry Understanding Membrane Protein Drug Targets in Computational Perspective
Current Drug Targets Protective Effects of the Caffeine Against Neurodegenerative Diseases
Current Medicinal Chemistry Preface
Current Neuropharmacology Quetiapine and Valproic Acid-induced Central Hypothyroidism in a Patient with Autism Spectrum Disorder and Intractable Epilepsy: A Case Report
Endocrine, Metabolic & Immune Disorders - Drug Targets Parthenolide and its Analogues: A New Potential Strategy for the Treatment of Triple-Negative Breast Tumors
Current Medicinal Chemistry High Mobility Group Box-1 (HMGB1): A Potential Target in Therapeutics
Current Drug Targets ABC Transporters in the CNS – An Inventory
Current Pharmaceutical Biotechnology