Abstract
Epilepsy is one of the commonly occurring chronic neurological disorders which involves abnormal electrical impulses in the brain. It is characterized by the sudden loss of consciousness, followed by abnormal shaking of the body. Though there are various types of antiepileptic drugs available clinically, the treatment of epilepsy still remains inadequate because of their toxicity and idiosyncratic side effects. Thus, there is unmet medical need to develop safe drugs for the treatment of epilepsy with lower side effects and improved bioavailability profiles. Considering the structural similarity between phenytoin/lamotrigine, a series of 1,3,4-thiadiazole was designed based on molecular docking study into the active site of the voltage-gated sodium channels. Antiepileptic activity of the synthesized compounds was evaluated in rats by maximal electroshock induced seizures (MES) model at different doses. Among the tested compounds, some exhibited significant anticonvulsant activity as compared to phenytoin in a dose-dependent manner. The neurotoxicity study was carried out using the rotarod test and the results of which suggests that the target compounds are safe and could be further developed as potential lead for antiepileptic drugs.
Keywords: Antiepileptic activity, docking study, epilepsy, green synthesis, neurotoxicity, thiadiazole.
Mini-Reviews in Medicinal Chemistry
Title:Molecular Docking Study, Green Synthesis and Pharmacological Evaluation of 1,3,4-thiadiazole Derivatives as Potential Antiepileptic Agents
Volume: 13 Issue: 14
Author(s): Biswa Mohan Sahoo, S. C. Dinda, B. V.V. Ravi Kumar, J. R. Panda and Pathik S. Brahmkshatriya
Affiliation:
Keywords: Antiepileptic activity, docking study, epilepsy, green synthesis, neurotoxicity, thiadiazole.
Abstract: Epilepsy is one of the commonly occurring chronic neurological disorders which involves abnormal electrical impulses in the brain. It is characterized by the sudden loss of consciousness, followed by abnormal shaking of the body. Though there are various types of antiepileptic drugs available clinically, the treatment of epilepsy still remains inadequate because of their toxicity and idiosyncratic side effects. Thus, there is unmet medical need to develop safe drugs for the treatment of epilepsy with lower side effects and improved bioavailability profiles. Considering the structural similarity between phenytoin/lamotrigine, a series of 1,3,4-thiadiazole was designed based on molecular docking study into the active site of the voltage-gated sodium channels. Antiepileptic activity of the synthesized compounds was evaluated in rats by maximal electroshock induced seizures (MES) model at different doses. Among the tested compounds, some exhibited significant anticonvulsant activity as compared to phenytoin in a dose-dependent manner. The neurotoxicity study was carried out using the rotarod test and the results of which suggests that the target compounds are safe and could be further developed as potential lead for antiepileptic drugs.
Export Options
About this article
Cite this article as:
Sahoo Mohan Biswa, Dinda C. S., Kumar V.V. Ravi B., Panda R. J. and Brahmkshatriya S. Pathik, Molecular Docking Study, Green Synthesis and Pharmacological Evaluation of 1,3,4-thiadiazole Derivatives as Potential Antiepileptic Agents, Mini-Reviews in Medicinal Chemistry 2013; 13 (14) . https://dx.doi.org/10.2174/13895575113136660099
DOI https://dx.doi.org/10.2174/13895575113136660099 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
Call for Papers in Thematic Issues
Bioprospecting of Natural Products as Sources of New Multitarget Therapies
According to the Convention on Biological Diversity, bioprospecting is the exploration of biodiversity and indigenous knowledge to develop commercially valuable products for pharmaceutical and other applications. Bioprospecting involves searching for useful organic compounds in plants, fungi, marine organisms, and microorganisms. Natural products traditionally constituted the primary source of more than ...read more
Computational Frontiers in Medicinal Chemistry
The thematic issue "Computational Frontiers in Medicinal Chemistry" provides a robust platform for delving into state-of-the-art computational methodologies and technologies that significantly propel advancements in medicinal chemistry. This edition seeks to amalgamate top-tier reviews spotlighting the latest trends and breakthroughs in the fusion of computational approaches, including artificial intelligence (AI) ...read more
Natural Products and Dietary Supplements in Alleviation of Metabolic, Cardiovascular, and Neurological Disorders
Metabolic disorders like diabetes, obesity, inflammation, oxidative stress, cancer etc, cardiovascular disorders like angina, myocardial infarction, congestive heart failure etc as well as neurological disorders like Alzheimer?s, Parkinson?s, Epilepsy, Depression, etc are the global burden. They covered the major segment of the diseases and disorders from which the human community ...read more
Natural Products in Drug Discovery
Natural products have always been one of the important ways of drug discovery due to their novel skeleton and diverse functional group characteristics. According to statistics, between 1981 and 2019, the FDA approved a total of 1,394 small molecule drugs for marketing, of which 930 marketed drugs originated from the ...read more
- 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
-
Characterization of Single Nucleotide Polymorphisms of Cytochrome P450 in an Australian Deceased Sample
Current Drug Metabolism Cm38: A New Antimicrobial Peptide Active Against Klebsiella pneumoniae is Homologous to Cn11
Protein & Peptide Letters Novel Therapeutic Strategies for Dementia
CNS & Neurological Disorders - Drug Targets Mevalonate Cascade and Neurodevelopmental and Neurodegenerative Diseases: Future Targets for Therapeutic Application
Current Molecular Pharmacology Approaching Neurological Diseases to Reduce Mobility Limitations in Older Persons
Current Pharmaceutical Design Small Peptide and Protein-based Molecular Probes for Imaging Neurological Diseases
Current Protein & Peptide Science 5'-Nucleotidases, Nucleosides and their Distribution in the Brain: Pathological and Therapeutic Implications
Current Medicinal Chemistry Raf Inhibitors as Therapeutic Agents Against Neurodegenerative Diseases
CNS & Neurological Disorders - Drug Targets MicroRNAs Involved in Oxidative Stress Processes Regulating Physiological and Pathological Responses
MicroRNA Multi-Target-Directed Ligands Affecting Serotonergic Neurotransmission for Alzheimer’s Disease Therapy: Advances in Chemical and Biological Research
Current Medicinal Chemistry The Clinics and Etiology of Preeclampsia
Current Women`s Health Reviews Antiepileptogenic Effect of Retinoic Acid
Current Neuropharmacology Clinical Pharmacology of Phenobarbital in Neonates: Effects, Metabolism and Pharmacokinetics
Current Pediatric Reviews Structure-to-function Relationship of Carbohydrates in the Mechanism of Lysosomal Storage Disorders (LSDs)
Current Organic Chemistry Neuro-Transmitters in the Central Nervous System & their Implication in Learning and Memory Processes
Current Medicinal Chemistry Epilepsy, Comorbidities and Treatments
Current Pharmaceutical Design Optimization of the Enzymolysis Conditions for Scorpion Peptides and Evaluation of its Antitumor Activity
Current Signal Transduction Therapy Molecular Targets of Cannabinoids Associated with Depression
Current Medicinal Chemistry Editorial [Hot Topic: Neurotransmitter Transporters Guest Editor: Dr. Anders A. Jensen ]
Current Topics in Medicinal Chemistry Towards the Molecular Foundations of Glutamatergic-targeted Antidepressants
Current Neuropharmacology