Abstract
A series of 6-alkoxy-2-(4H-1,2,4-triazol-4-yl)benzothiazoles was synthesized and evaluated for their anticonvulsant activity using the maximal electroshock (MES) method. Interestingly, all of the compounds prepared showed long duration of protection effect in the MES screens. And none of them, except compounds 4b and 4d, showed any neurotoxicity at dose of 300 mg/kg. Compound 4c was considered as the most promising one with an ED50 value of 39.4 mg/kg, and a superior PI value of 17.3 when compared to the marketed antiepileptic drugs carbamazepine, phenobarbital, and valproate. What’s more, compound 4c showed high protection against seizures induced by pentylenetetrazole.
Keywords: Anticonvulsant, Benzothiazole, MES, Neurotoxicity, Rotorod, Triazole.
Letters in Drug Design & Discovery
Title:Synthesis and Evaluation of Anticonvulsant Activities of Triazole- Incorporated Benzothiazoles
Volume: 11 Issue: 4
Author(s): Ming-Xia Song, Hong Zeng, Xian-Qing Deng and Zhe-Shan Quan
Affiliation:
Keywords: Anticonvulsant, Benzothiazole, MES, Neurotoxicity, Rotorod, Triazole.
Abstract: A series of 6-alkoxy-2-(4H-1,2,4-triazol-4-yl)benzothiazoles was synthesized and evaluated for their anticonvulsant activity using the maximal electroshock (MES) method. Interestingly, all of the compounds prepared showed long duration of protection effect in the MES screens. And none of them, except compounds 4b and 4d, showed any neurotoxicity at dose of 300 mg/kg. Compound 4c was considered as the most promising one with an ED50 value of 39.4 mg/kg, and a superior PI value of 17.3 when compared to the marketed antiepileptic drugs carbamazepine, phenobarbital, and valproate. What’s more, compound 4c showed high protection against seizures induced by pentylenetetrazole.
Export Options
About this article
Cite this article as:
Song Ming-Xia, Zeng Hong, Deng Xian-Qing and Quan Zhe-Shan, Synthesis and Evaluation of Anticonvulsant Activities of Triazole- Incorporated Benzothiazoles, Letters in Drug Design & Discovery 2014; 11 (4) . https://dx.doi.org/10.2174/15701808113106660093
DOI https://dx.doi.org/10.2174/15701808113106660093 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
- 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
-
Adaptive Behavior in Williams-Beuren Syndrome, Down Syndrome, and Autism Spectrum Disorder
Current Psychiatry Reviews Targeting Cancer Stem Cells with Repurposed Drugs to Improve Current Therapies
Recent Patents on Anti-Cancer Drug Discovery Clinical Pharmacogenetics and Potential Application in Personalized Medicine
Current Drug Metabolism The Role of <i>Eif2s3y</i> in Mouse Spermatogenesis and ESC
Current Stem Cell Research & Therapy Opioids and the Blood-Brain Barrier: A Dynamic Interaction with Consequences on Drug Disposition in Brain
Current Neuropharmacology Pharmacological Strategies for Neuroprotection in Traumatic Brain Injury
Mini-Reviews in Medicinal Chemistry Current Methods in the Automatic Tissue Segmentation of 3D Magnetic Resonance Brain Images
Current Medical Imaging Development and Evaluation of an Anti-Epileptic Oral Fast-Dissolving Film with Enhanced Dissolution and In vivo Permeation
Current Drug Delivery Signaling Pathways that Regulate Basal ABC Transporter Activity at the Blood- Brain Barrier
Current Pharmaceutical Design Unusual Clinical Manifestations of the Antiphospholipid Syndrome
Current Rheumatology Reviews Status Analysis of Herbal Drug Therapies in Epilepsy: Advancements in the Use of Medicinal Plants with Anti-inflammatory Properties
Combinatorial Chemistry & High Throughput Screening Genetics of Serotonin Receptors and Depression: State of the Art
Current Drug Targets Adenosine Receptors: What We Know and What We are Learning
Current Topics in Medicinal Chemistry Cytotoxicity and Anti-proliferative Properties of Heterocyclic Compounds Derived from Progesterone
Anti-Cancer Agents in Medicinal Chemistry Examination of Hippocampal Differences Between Alzheimer Disease, Amnestic Mild Cognitive Impairment and Normal Aging: Diffusion Kurtosis
Current Alzheimer Research Thymoquinone: Major Molecular Targets, Prominent Pharmacological Actions and Drug Delivery Concerns
Current Bioactive Compounds Preface:
Recent Patents and Topics on Imaging (Discontinued) In Silico Validation and Structure Activity Relationship Study of a Series of Pyridine-3-carbohydrazide Derivatives as Potential Anticonvulsants in Generalized and Partial Seizures
Central Nervous System Agents in Medicinal Chemistry Editorial (Thematic Issue: Linkage of Neurodegenerative Disorders with Other Health Issues – Volume I)
CNS & Neurological Disorders - Drug Targets Repetitive Transcranial Magnetic Stimulation for ALS
CNS & Neurological Disorders - Drug Targets