Abstract
A series of novel (±) 3-menthone semicarbazides (1-7) and thiosemicarbazides (8-14) were synthesized using an appropriate synthetic route and characterized by thin layer chromatography and spectral analysis. The anticonvulsant activity of synthesized compounds was established after intraperitoneal administration in three seizure models in mice which include maximal electroshock seizure (MES), subcutaneous pentylene tetrazole (scPTZ) induced seizure and minimal neurotoxicity test. Seven compounds exhibited protection in both models and N1 – (4-fluorophenyl) – N4- (menth-3- one) semicarbazide (4) emerged as the most active compound with MES ED50 of 44.15mg/kg and scPTZ ED50 of 38.68mg/kg at 0.25h duration. These compounds were found to elevate γ-amino butyric acid (GABA) levels in the midbrain region, thus indicating that (±) 3-menthone semicarbazides could be considered as a lead molecule in designing of a potent anticonvulsant drug.
Keywords: (±) 3-menthone, semicarbazides, thiosemicarbazides, anticonvulsant, Maximal Electroshock Seizure (MES), subcutaneous pentylene tetrazole (scPTZ), Antiepileptic drug development (AED)
Medicinal Chemistry
Title: Menthone Semicarbazides and Thiosemicarbazides as Anticonvulsant Agents
Volume: 6 Issue: 1
Author(s): Jainendra Jain, Y. Kumar, James Stables and Reema Sinha
Affiliation:
Keywords: (±) 3-menthone, semicarbazides, thiosemicarbazides, anticonvulsant, Maximal Electroshock Seizure (MES), subcutaneous pentylene tetrazole (scPTZ), Antiepileptic drug development (AED)
Abstract: A series of novel (±) 3-menthone semicarbazides (1-7) and thiosemicarbazides (8-14) were synthesized using an appropriate synthetic route and characterized by thin layer chromatography and spectral analysis. The anticonvulsant activity of synthesized compounds was established after intraperitoneal administration in three seizure models in mice which include maximal electroshock seizure (MES), subcutaneous pentylene tetrazole (scPTZ) induced seizure and minimal neurotoxicity test. Seven compounds exhibited protection in both models and N1 – (4-fluorophenyl) – N4- (menth-3- one) semicarbazide (4) emerged as the most active compound with MES ED50 of 44.15mg/kg and scPTZ ED50 of 38.68mg/kg at 0.25h duration. These compounds were found to elevate γ-amino butyric acid (GABA) levels in the midbrain region, thus indicating that (±) 3-menthone semicarbazides could be considered as a lead molecule in designing of a potent anticonvulsant drug.
Export Options
About this article
Cite this article as:
Jain Jainendra, Kumar Y., Stables James and Sinha Reema, Menthone Semicarbazides and Thiosemicarbazides as Anticonvulsant Agents, Medicinal Chemistry 2010; 6 (1) . https://dx.doi.org/10.2174/157340610791208727
DOI https://dx.doi.org/10.2174/157340610791208727 |
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
-
Therapeutic Trials in Human Transmissible Spongiform Encephalopathies: Recent Advances and Problems to Address
Infectious Disorders - Drug Targets Update on the Evaluation and Management of Brief Resolved Unexplained Events (Previously Apparent Life-Threatening Events)
Reviews on Recent Clinical Trials Management of Antiepileptic Treatment After Epilepsy Surgery - Practices and Problems
Current Pharmaceutical Design Anticonvulsant and Neurotoxicity of Some Novel 1-([1,3,4]thiadiazino[6,5- b]indol-3-yl Semicarbazides
Central Nervous System Agents in Medicinal Chemistry Bryostatin-1 Synergizes with Histone Deacetylase Inhibitors to Reactivate HIV-1 from Latency
Current HIV Research Supplements, Diets and Other Complementary and Alternative Interventions in Adolescent Mental Health
Adolescent Psychiatry Search for Molecular Basis of Antifungal Activity of Thiosemicarbazide Derivatives: A Combined in vitro Antifungal and Enzymatic Studies with in Silico Docking
Letters in Drug Design & Discovery Neurotransmitters and Chemokines Regulate Tumor Cell Migration: Potential for a New Pharmacological Approach to Inhibit Invasion and Metastasis Development
Current Pharmaceutical Design GABA Receptors: Pharmacological Potential and Pitfalls
Current Pharmaceutical Design Unexpected Effects of Acetylcholine Precursors on Pilocarpine Seizure- Induced Neuronal Death
Current Neuropharmacology Advantages of Structure-Based Drug Design Approaches in Neurological Disorders
Current Neuropharmacology PLGA Nanoparticles for Nose to Brain Delivery of Clonazepam: Formulation, Optimization by 32 Factorial Design, In Vitro and In Vivo Evaluation
Current Drug Delivery The Glial Sodium-Calcium Exchanger: A New Target for Nitric Oxide- Mediated Cellular Toxicity
Current Protein & Peptide Science Cardiovascular effect of Nigella sativa L. Aqueous Extract in Normal Rats
Cardiovascular & Hematological Disorders-Drug Targets Subject Index To Volume 9
Current Medicinal Chemistry Novel Histone Deacetylase Inhibitors for the Treatment of Pediatric Brain Tumors
Central Nervous System Agents in Medicinal Chemistry Integration of Pharmacogenomics and Pharmacometrics to Support Drug Development, Regulatory and Therapeutic Decisions
Current Pharmacogenomics and Personalized Medicine Mitochondrial Permeability Transition Pore as a Suitable Targ e t for Neuroprotective Agents Against Alzheimer’s Disease
CNS & Neurological Disorders - Drug Targets Anticonvulsant Action and Long-term Effects of Gabapentin
Current Neuropharmacology Structure, Roles and Inhibitors of a Mitotic Protein Kinase Haspin
Current Medicinal Chemistry