Abstract
A series of 4-butyl-5-(4-alkoxyphenyl)-2H-1,2,4-triazole-3(4H)-ones (6a-6u) was designed and synthesized. The anticonvulsant effects and neurotoxicity of the compounds were evaluated with maximal electroshock test and rotarod test. Among the synthetic compounds, 4-butyl-5-(4-(2-fluorinebenzyl)phenyl)-2H-1,2,4-triazole-3 (4H)-one (6k) was the most potent with ED50 value of 27.4 mg/kg and protective index (PI = TD50/ED50) value of 12.0. Besides the anti-MES efficacy, the potency of compound 6k against seizures induced by pentylenetetrazole (PTZ), 3-mercaptopropionic acid (3- MP), and bicuculline (BIC) was also established, which suggested that the mechanisms of action including enhancing of GABAergic activity might be involved in its anticonvulsant activity.
Keywords: Anticonvulsant, GABA, Maximal electroshock test, Neurotoxicity, Synthesis, Triazolone.
Letters in Drug Design & Discovery
Title:Synthesis and Anticonvulsant Activity Evaluation of 4-butyl-5-(4- alkoxyphenyl)-2H-1,2,4-triazole-3(4H)-ones
Volume: 11 Issue: 5
Author(s): Zi-Shi Zhu, Shi-Ben Wang, Xian-Qing Deng, Da-Chuan Liu and Zhe-Shan Quan
Affiliation:
Keywords: Anticonvulsant, GABA, Maximal electroshock test, Neurotoxicity, Synthesis, Triazolone.
Abstract: A series of 4-butyl-5-(4-alkoxyphenyl)-2H-1,2,4-triazole-3(4H)-ones (6a-6u) was designed and synthesized. The anticonvulsant effects and neurotoxicity of the compounds were evaluated with maximal electroshock test and rotarod test. Among the synthetic compounds, 4-butyl-5-(4-(2-fluorinebenzyl)phenyl)-2H-1,2,4-triazole-3 (4H)-one (6k) was the most potent with ED50 value of 27.4 mg/kg and protective index (PI = TD50/ED50) value of 12.0. Besides the anti-MES efficacy, the potency of compound 6k against seizures induced by pentylenetetrazole (PTZ), 3-mercaptopropionic acid (3- MP), and bicuculline (BIC) was also established, which suggested that the mechanisms of action including enhancing of GABAergic activity might be involved in its anticonvulsant activity.
Export Options
About this article
Cite this article as:
Zhu Zi-Shi, Wang Shi-Ben, Deng Xian-Qing, Liu Da-Chuan and Quan Zhe-Shan, Synthesis and Anticonvulsant Activity Evaluation of 4-butyl-5-(4- alkoxyphenyl)-2H-1,2,4-triazole-3(4H)-ones, Letters in Drug Design & Discovery 2014; 11 (5) . https://dx.doi.org/10.2174/1570180810666131122003939
DOI https://dx.doi.org/10.2174/1570180810666131122003939 |
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
-
Cardiovascular effect of Nigella sativa L. Aqueous Extract in Normal Rats
Cardiovascular & Hematological Disorders-Drug Targets A Randomized, Double-Blind, Placebo-Controlled Pilot Trial of Safety and Tolerability of Two Doses of Divalproex Sodium in Outpatients with Probable Alzheimers Disease
Current Alzheimer Research Screen-Printed Biosensors in Drug Analysis
Current Pharmaceutical Analysis Possible Exploitation of Non-Neuronal and Non-Chemical Synaptic Signalling Pathways in Epilepsy Therapy
Current Signal Transduction Therapy Intracellular and Extracellular Zinc Detection by Organic Fluorescent Receptor
Current Organic Chemistry Genetic Variation of Chromosome 1q42: Etiologic Mechanism of Congenital Disorders of Neuronal Migration and Synaptogenesis
Current Psychiatry Reviews Structure-Based Design of Benzimidazole Sugar Conjugates: Synthesis, SAR and In Vivo Anti-inflammatory and Analgesic Activities
Medicinal Chemistry Teratogenic Potential of Atypical Antipsychotic Drugs, Quetiapine and Aripiprazole in Rats
Current Psychopharmacology Non-Imidazole Histamine H3 Ligands. Part VI. Synthesis and Preliminary Pharmacological Investigation of Thiazole-Type Histamine H3-Receptor Antagonists with Lacking a Nitrogen Nucleus in the Side Chain
Medicinal Chemistry Distinct Forms of Spinal Cysticercosis: A Vietnamese Case Series
Current Medical Imaging Anesthetics as Chemical Tools to Study the Structure and Function of Nicotinic Acetylcholine Receptors
Current Protein & Peptide Science Ghrelin as a Neuroprotective and Palliative Agent in Alzheimer's and Parkinson's Disease
Current Pharmaceutical Design Characterization of Single Nucleotide Polymorphisms of Cytochrome P450 in an Australian Deceased Sample
Current Drug Metabolism A Multi-Functional Organelle Mitochondrion is Involved in Cell Death, Proliferation and Disease
Current Medicinal Chemistry Central and Peripheral Pain Generators in Women with Chronic Pelvic Pain: Patient Centered Assessment and Treatment
Current Rheumatology Reviews Safety of Inhaled Corticosteroids. Why the Variation in Systemic Adverse Effects?
Current Pediatric Reviews Understanding Effects of Psychological Stress on Physiology and Disease Through Human Stressome - An Integral Algorithm
Current Bioinformatics A Review of Recent Patents on the ASICs as a Key Drug Target
Recent Patents on Biotechnology Microemulsions and Nanoemulsions for Targeted Drug Delivery to the Brain
Current Nanoscience Patents on Non-Viral Mediated Gene Delivery
Recent Patents on DNA & Gene Sequences