Abstract
Background: 21 novel 1-alkoxy-1H-benzo[d]-1,2,3-triazole compounds were designed, prepared and evaluated for their antidepressant and anticonvulsant effects in mice.
Method: Compound 19 significantly decreased immobility time in the FST without altering the locomotor activity in the open field test, and exhibited higher levels of efficacy than the reference standard fluoxetine. Compound 19 significantly increased 5-HT, NE and 5-HIAA levels in mice brain, implying that the antidepressant activity might be mediated by these neurotransmitters. In the seizure test, compound 19 also showed better anticonvulsant activity against MES, whereas had not shown neurotoxicity (300 mg/kg). Conclusion: Our data indicated that compound 19 could potentially be used as the antidepressant drug in patients with epilepsy.Keywords: Benzo[d]-1, 2, 3-triazole, FST, neurotransmitters, MES, antidepressant.
Letters in Drug Design & Discovery
Title:Design, Synthesis and Antidepressant and Anticonvulsant Effect of 1-Alkoxy-1H-Benzo[d]-1,2,3-Triazole Derivatives
Volume: 14 Issue: 3
Author(s): Yu Sun, Qing-Hao Jin, Yan Han, Di Yu, Qiu-Ping Dai and Zhou-Jun Zheng
Affiliation:
Keywords: Benzo[d]-1, 2, 3-triazole, FST, neurotransmitters, MES, antidepressant.
Abstract: Background: 21 novel 1-alkoxy-1H-benzo[d]-1,2,3-triazole compounds were designed, prepared and evaluated for their antidepressant and anticonvulsant effects in mice.
Method: Compound 19 significantly decreased immobility time in the FST without altering the locomotor activity in the open field test, and exhibited higher levels of efficacy than the reference standard fluoxetine. Compound 19 significantly increased 5-HT, NE and 5-HIAA levels in mice brain, implying that the antidepressant activity might be mediated by these neurotransmitters. In the seizure test, compound 19 also showed better anticonvulsant activity against MES, whereas had not shown neurotoxicity (300 mg/kg). Conclusion: Our data indicated that compound 19 could potentially be used as the antidepressant drug in patients with epilepsy.Export Options
About this article
Cite this article as:
Sun Yu, Jin Qing-Hao, Han Yan, Yu Di, Dai Qiu-Ping and Zheng Zhou-Jun, Design, Synthesis and Antidepressant and Anticonvulsant Effect of 1-Alkoxy-1H-Benzo[d]-1,2,3-Triazole Derivatives, Letters in Drug Design & Discovery 2017; 14 (3) . https://dx.doi.org/10.2174/1570180813666160826113018
DOI https://dx.doi.org/10.2174/1570180813666160826113018 |
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
-
Stem Cell Ageing and Apoptosis
Current Pharmaceutical Design Neonatal Atlas Templates for the Study of Brain Development Using Magnetic Resonance Images
Current Medical Imaging 3,4-DHQLO and Triazole and Its Related Analogues with Anticonvulsant Effects
Mini-Reviews in Medicinal Chemistry Obstructive Sleep Apnea Syndrome: From Phenotype to Genetic Basis
Current Genomics TRP Channels: New Potential Therapeutic Approaches in CNS Neuropathies
CNS & Neurological Disorders - Drug Targets Imidazole: An Essential Edifice for the Identification of New Lead Compounds and Drug Development
Mini-Reviews in Medicinal Chemistry Bipolar Affective Disorder, Epilepsy and Migraine – Does Possible Shared Pathogenesis Explain their Association?
Current Psychopharmacology Incorporating Natural Products, Pharmaceutical Drugs, Self-Care and Digital/Mobile Health Technologies into Molecular-Behavioral Combination Therapies for Chronic Diseases
Current Clinical Pharmacology Selenium Deficiency in Soils and Crops and its Impact on Animal and Human Health
Current Nutrition & Food Science Recent Advances in the Discovery of α1-Adrenoceptor Agonists
Current Topics in Medicinal Chemistry Transgenic Mice as a Model for Alzheimers Disease
Current Alzheimer Research Computational Study and Synthesis of a New Class of Anticonvulsants with 6 Hz Psychomotor Seizure Test Activity: 2-(1,3-benzodioxol-5-yloxy)- N'-[substituted]-acetohydrazides
Medicinal Chemistry Perspective on mTOR-dependent Protection in Status Epilepticus
Current Neuropharmacology Structure of Glutamate Receptors
Current Drug Targets Induction of Nuclear Receptors and Drug Resistance in the Brain Microvascular Endothelial Cells Treated with Antiepileptic Drugs
Current Neurovascular Research Recent Advances in the Modulation of Voltage-Gated Ion Channels for the Treatment of Epilepsy
Current Drug Targets - CNS & Neurological Disorders Opioids and the Blood-Brain Barrier: A Dynamic Interaction with Consequences on Drug Disposition in Brain
Current Neuropharmacology Patent Annotations
Recent Patents on CNS Drug Discovery (Discontinued) Preface
Current Pharmaceutical Design Cell-based Treatment of Cerebral Palsy: Still a Long Way Ahead
Current Stem Cell Research & Therapy