Abstract
A series of novel 1-benzhydryl-4-(3-(piperidin-4-yl)propyl)piperidine sulphonamide derivatives 8(a-j) was synthesized in good yield and met the structural requirements essential for anticonvulsant properties. The structures of the synthesized compounds were confirmed on the basis of their spectral data and elemental analysis. All the compounds were evaluated for their possible anticonvulsant activity by Maximal Electroshock Seizure (MES) test and their neurotoxic effects were determined by rotorod test. Majority of the compounds were active in MES tests. Compounds 8f and 8g have shown a significant and protective effect on seizure, when compared with standard drug phenytoin. Compound 8f and 8g without a fluoro group showed anticonvulsant activity in MES test as compared with compound 8a and 8b with fluoro substituents. From this study, it is quite apparent that there are at least three parameters for the activity of anticonvulsant drugs, that is, a lipophilic domain, a distal hydrophobic center and two-electron donor (-C-N=) system.
Keywords: Benzhydryl chloride, Sulfonyl chloride, Anticonvulsant, Convulsiometer, Epilepsy
Letters in Drug Design & Discovery
Title: Synthesis of Novel 1-benzhydryl-4-(3-(piperidin-4-yl)propyl) Piperidine Sulfonamides as Anticonvulsant Agents
Volume: 7 Issue: 2
Author(s): K. Vinaya, B. Veeresh, C. S. Ananda Kumar, D. S. Prasanna, S. R. Ranganatha, S. B. Benaka Prasad, B. M. Patil and K. S. Rangappa
Affiliation:
Keywords: Benzhydryl chloride, Sulfonyl chloride, Anticonvulsant, Convulsiometer, Epilepsy
Abstract: A series of novel 1-benzhydryl-4-(3-(piperidin-4-yl)propyl)piperidine sulphonamide derivatives 8(a-j) was synthesized in good yield and met the structural requirements essential for anticonvulsant properties. The structures of the synthesized compounds were confirmed on the basis of their spectral data and elemental analysis. All the compounds were evaluated for their possible anticonvulsant activity by Maximal Electroshock Seizure (MES) test and their neurotoxic effects were determined by rotorod test. Majority of the compounds were active in MES tests. Compounds 8f and 8g have shown a significant and protective effect on seizure, when compared with standard drug phenytoin. Compound 8f and 8g without a fluoro group showed anticonvulsant activity in MES test as compared with compound 8a and 8b with fluoro substituents. From this study, it is quite apparent that there are at least three parameters for the activity of anticonvulsant drugs, that is, a lipophilic domain, a distal hydrophobic center and two-electron donor (-C-N=) system.
Export Options
About this article
Cite this article as:
Vinaya K., Veeresh B., Ananda Kumar S. C., Prasanna S. D., Ranganatha R. S., Benaka Prasad B. S., Patil M. B. and Rangappa S. K., Synthesis of Novel 1-benzhydryl-4-(3-(piperidin-4-yl)propyl) Piperidine Sulfonamides as Anticonvulsant Agents, Letters in Drug Design & Discovery 2010; 7 (2) . https://dx.doi.org/10.2174/157018010790225868
DOI https://dx.doi.org/10.2174/157018010790225868 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
![](/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
-
Therapeutic Efficacy of Selegiline in Neurodegenerative Disorders and Neurological Diseases
Current Drug Targets Hypothesis-Driven Medication Discovery for the Treatment of Psychostimulant Addiction
Current Drug Abuse Reviews Targeted Toxins for Glioblastoma Multiforme: Pre-Clinical Studies and Clinical Implementation
Anti-Cancer Agents in Medicinal Chemistry Transforming Growth Factor-β Signaling in Motor Neuron Diseases
Current Molecular Medicine Mind-Body Practices and the Adolescent Brain: Clinical Neuroimaging Studies
Adolescent Psychiatry Genetic Studies on the Role of T-Type Ca2+ Channels in Sleep and Absence Epilepsy
CNS & Neurological Disorders - Drug Targets Relevance of Follow-Up in Patients with Core Clinical Criteria for Alzheimer Disease and Normal CSF Biomarkers
Current Alzheimer Research Advances in the Understanding of the Gabaergic Neurobiology of FMR1 Expanded Alleles Leading to Targeted Treatments for Fragile X Spectrum Disorder
Current Pharmaceutical Design Use of Bromine-76 and Iodine-123 Radiohalogenated Tracers in the Drug Development Process
Current Pharmaceutical Design Alkaloids as Important Scaffolds in Therapeutic Drugs for the Treatments of Cancer, Tuberculosis, and Smoking Cessation
Current Topics in Medicinal Chemistry Pathophysiogenesis of Mesial Temporal Lobe Epilepsy: Is Prevention of Damage Antiepileptogenic?
Current Medicinal Chemistry Potential Health Benefits of Passion Fruit Peel Flour
The Natural Products Journal Understanding the Potential Role and Delivery Approaches of Nitric Oxide in Chronic Wound Healing Management
Current Pharmaceutical Design Resveratrol in Medicinal Chemistry: A Critical Review of its Pharmacokinetics, Drug-Delivery, and Membrane Interactions
Current Medicinal Chemistry Ongoing Electroencephalographic Activity Associated with Cortical Arousal in Transgenic PDAPP Mice (hAPP V717F)
Current Alzheimer Research Meet Our Editorial Board Member
Current Neuropharmacology Preface
Current Neuropharmacology Triheptanoin Supplementation to Ketogenic Diet Curbs Cognitive Impairment in APP/PS1 Mice Used as a Model of Familial Alzheimer’s Disease
Current Alzheimer Research Fibromyalgia: Mechanisms, Current Treatment and Animal Models
Current Pharmaceutical Biotechnology Therapeutic Role of Zonisamide in Neuropsychiatric Disorders
Mini-Reviews in Medicinal Chemistry