Abstract
A series of novel imidazole incorporated semicarbazones was synthesized using an appropriate synthetic route and characterized by spectral analysis (IR, 1H NMR, 13C NMR and Mass). The anticonvulsant activity of the synthesized compounds was determined using doses of 30, 100, and 300 mg kg-1 against maximal electroshock seizure (MES), subcutaneous pentylenetetrazole (scPTZ) induced seizure and minimal neurotoxicity test. Six compounds exhibited protection in both models and 2-(1-(4-chlorophenyl)-2-(1H-imidazol-1-yl)ethylidene)-N-p-tolylsemicarbazone emerged as the most active compound of the series without any neurotoxicity and significant CNS depressant effect. Liver enzyme estimations (SGOT, SGPT, Alkaline phosphatase) of the compound also showed no significant change in the enzymes levels. Moreover, it caused 80% elevation of γ-amino butyric acid (GABA) levels in the whole mice brain, thus indicating that it could be a promising candidate in designing of a potent anticonvulsant drug.
Keywords: Anticonvulsants, Semicarbazone, Imidazole, GABA
Medicinal Chemistry
Title:Imidazole Incorporated Semicarbazone Derivatives as a New Class of Anticonvulsants: Design, Synthesis and In-Vivo Screening
Volume: 9 Issue: 4
Author(s): Mohammad Amir, Israr Ali and Mohd. Zaheen Hassan
Affiliation:
Keywords: Anticonvulsants, Semicarbazone, Imidazole, GABA
Abstract: A series of novel imidazole incorporated semicarbazones was synthesized using an appropriate synthetic route and characterized by spectral analysis (IR, 1H NMR, 13C NMR and Mass). The anticonvulsant activity of the synthesized compounds was determined using doses of 30, 100, and 300 mg kg-1 against maximal electroshock seizure (MES), subcutaneous pentylenetetrazole (scPTZ) induced seizure and minimal neurotoxicity test. Six compounds exhibited protection in both models and 2-(1-(4-chlorophenyl)-2-(1H-imidazol-1-yl)ethylidene)-N-p-tolylsemicarbazone emerged as the most active compound of the series without any neurotoxicity and significant CNS depressant effect. Liver enzyme estimations (SGOT, SGPT, Alkaline phosphatase) of the compound also showed no significant change in the enzymes levels. Moreover, it caused 80% elevation of γ-amino butyric acid (GABA) levels in the whole mice brain, thus indicating that it could be a promising candidate in designing of a potent anticonvulsant drug.
Export Options
About this article
Cite this article as:
Amir Mohammad, Ali Israr and Zaheen Hassan Mohd., Imidazole Incorporated Semicarbazone Derivatives as a New Class of Anticonvulsants: Design, Synthesis and In-Vivo Screening, Medicinal Chemistry 2013; 9 (4) . https://dx.doi.org/10.2174/1573406411309040011
DOI https://dx.doi.org/10.2174/1573406411309040011 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
- 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
-
From Discovery to Clinical Trials: Treatment Strategies for Central Neuropathic Pain after Spinal Cord Injury
Current Pharmaceutical Design Antiepileptic Drugs Based on the α-Substituted Amide Group Pharmacophore: From Chemical Crystallography to Molecular Pharmaceutics
Current Pharmaceutical Design Codon Usage Biases in Alzheimers Disease and Other Neurodegenerative Diseases
Protein & Peptide Letters The Quest for Eldorado: Development of Radioligands for In Vivo Imaging of Nicotinic Acetylcholine Receptors in Human Brain
Current Pharmaceutical Design MicroRNA-451 Aggravates Kainic Acid-induced Seizure and Neuronal Apoptosis by Targeting GDNF
Current Neurovascular Research Pharmacogenetics and Anaesthesiology
Current Pharmacogenomics The Role of SPECT and MRI for Pre and Postoperative Evaluation of Childhood Moyamoya Disease: Case Report and Review of Literature
Current Medical Imaging The Role of P-Glycoprotein in Psychiatric Disorders: A Reliable Guard of the Brain?
Central Nervous System Agents in Medicinal Chemistry Longitudinal Functional MRI of Motor and Cognitive Recovery Following Stroke: A Review
Current Medical Imaging Chemistry and Biological Activities of 1,3-Benzoxathiol-2-ones
Mini-Reviews in Organic Chemistry Poly(ADP-Ribose)Polymerase 1 (PARP-1) Activation and Ca<sup>2+</sup> Permeable α-Amino-3-Hydroxy-5-Methyl-4-Isoxazolepropionic Acid (AMPA) Channels in Post-Ischemic Brain Damage: New Therapeutic Opportunities?
CNS & Neurological Disorders - Drug Targets Development of Polymeric Nanocarriers for Brain Targeted Delivery of Atorvastatin: A Quality-By-Design Approach
Drug Delivery Letters In Silico Studies in Drug Research Against Neurodegenerative Diseases
Current Neuropharmacology Pathogenesis and Subtype of Intracerebral Hemorrhage (ICH) and ICH Score Determines Prognosis
Current Neurovascular Research GABA System as a Target for New Drugs
Current Medicinal Chemistry Patients Stratification Strategies to Optimize the Effectiveness of Scavenging Biogenic Aldehydes: Towards a Neuroprotective Approach for Parkinson's Disease
Current Neuropharmacology Endocrine Abnormalities Induced by Antiepileptic Drugs
Current Pediatric Reviews Immune Responses to Adeno-Associated Virus Vectors
Current Gene Therapy Systematic Comparison of the Performance of Different 2D and 3D Ligand-Based Virtual Screening Methodologies to Discover Anticonvulsant Drugs
Combinatorial Chemistry & High Throughput Screening Serotonin Control of Dopaminergic Neurotransmission: Focus on 5-HT2 Receptors
Current Neuropharmacology