Abstract
Background & Objective: A series of novel 3-Substituted-1,3,4,5-Tetrahydro-2H-benzo [b] azepine-2-one Derivatives (4, 5, 7, 10, 12, 5a-j, 8a-e) were synthesized from 1,2,3,4-Tetrahydro-1- naphthalenone. The structures of these compounds were confirmed by IR, 1H NMR, 13C NMR, MASS spectra and elemental analysis. Their anticonvulsant activity was evaluated by the maximal electroshock (MES) test, subcutaneous pentylenetetrazol (scPTZ) test, and their neurotoxicity was evaluated by the rotarod neurotoxicity test. Compound 4 showed the maximum anticonvulsant activity against the maximal electroshock test (ED50=26.4, PI =3.2) and against the subcutaneous pentylenetetrazol test (ED50=40.2, PI =2.1).
Conclusion: Possible structure-activity relationship was discussed.
Keywords: Anticonvulsant activity, toxicity, benzotriazoloazepine, synthesis, pharmacological, maximal electroshock test.
CNS & Neurological Disorders - Drug Targets
Title:Synthesis and Anticonvulsant Activity of 3-(alkylamino, alkoxy)-1,3,4,5- Tetrahydro-2H-benzo [b] azepine-2-one Derivatives
Volume: 17 Issue: 6
Author(s): Xia Huang, Tie Chen, Rong-Bi Han and Feng-Yu Piao*
Affiliation:
- Department of Chemistry, College of Science, Yanbian University, Yanji 133002, Jilin Province,China
Keywords: Anticonvulsant activity, toxicity, benzotriazoloazepine, synthesis, pharmacological, maximal electroshock test.
Abstract: Background & Objective: A series of novel 3-Substituted-1,3,4,5-Tetrahydro-2H-benzo [b] azepine-2-one Derivatives (4, 5, 7, 10, 12, 5a-j, 8a-e) were synthesized from 1,2,3,4-Tetrahydro-1- naphthalenone. The structures of these compounds were confirmed by IR, 1H NMR, 13C NMR, MASS spectra and elemental analysis. Their anticonvulsant activity was evaluated by the maximal electroshock (MES) test, subcutaneous pentylenetetrazol (scPTZ) test, and their neurotoxicity was evaluated by the rotarod neurotoxicity test. Compound 4 showed the maximum anticonvulsant activity against the maximal electroshock test (ED50=26.4, PI =3.2) and against the subcutaneous pentylenetetrazol test (ED50=40.2, PI =2.1).
Conclusion: Possible structure-activity relationship was discussed.
Export Options
About this article
Cite this article as:
Huang Xia , Chen Tie , Han Rong-Bi and Piao Feng-Yu *, Synthesis and Anticonvulsant Activity of 3-(alkylamino, alkoxy)-1,3,4,5- Tetrahydro-2H-benzo [b] azepine-2-one Derivatives, CNS & Neurological Disorders - Drug Targets 2018; 17 (6) . https://dx.doi.org/10.2174/1871527317666180704101332
DOI https://dx.doi.org/10.2174/1871527317666180704101332 |
Print ISSN 1871-5273 |
Publisher Name Bentham Science Publisher |
Online ISSN 1996-3181 |
Call for Papers in Thematic Issues
Diagnosis and treatment of central nervous system infectious diseases
Infectious diseases of the central nervous system (CNS) can be divided into bacterial, tuberculous, viral, fungal, parasitic infections, etc. Early etiological treatment is often the most crucial means to reduce the mortality rate of patients with central nervous system infections, reduce complications and sequelae, and improve prognosis. The initial clinical ...read more
Techniques of Drug Repurposing: Delivering a new life to Herbs & Drugs
Of late, with the adaptation of innovative approaches and integration of advancements made towards medical sciences as well as the availability of a wide range of tools; several therapeutic challenges are being translated into viable clinical solutions, with a high degree of efficacy, safety, and selectivity. With a better understanding ...read more
Trends and perspectives in the rational management of CNS disorders
Central nervous system (CNS) diseases enforce a significant global health burden, driving ongoing efforts to improve our understanding and effectiveness of therapy. This issue investigates current advances in the discipline, focusing on the understanding as well as therapeutic handling of various CNS diseases. The issue covers a variety of diseases, ...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
-
When Nutraceuticals Reinforce Drugs Side Effects: A Case Report
Current Drug Safety Tools in the Design of Therapeutic Drugs for CNS Disorders: An up-to-date Review
Current Molecular Pharmacology Policies to Prevent Tobacco Use and Exposure in Children, a Global Perspective
Current Pediatric Reviews Gene Therapy Approaches in an Autoimmune Demyelinating Disease: Multiple Sclerosis
Current Gene Therapy Anti-Androgen Drugs in the Treatment of Obsessive-Compulsive Disorder: A Systematic Review
Current Medicinal Chemistry Tau Silencing by siRNA in the P301S Mouse Model of Tauopathy
Current Gene Therapy Aerobic Nitroreduction by Flavoproteins: Enzyme Structure, Mechanisms and Role in Cancer Chemotherapy
Mini-Reviews in Medicinal Chemistry Medical Treatment of Gastrointestinal Stromal Tumors: State of the Art and Future Perspectives
Reviews on Recent Clinical Trials MiR-335-5p Inhibits β-Amyloid (Aβ) Accumulation to Attenuate Cognitive Deficits Through Targeting c-jun-N-terminal Kinase 3 in Alzheimer’s Disease
Current Neurovascular Research Complement Activation-Related Pseudoallergy Caused by Amphiphilic Drug Carriers: The Role of Lipoproteins
Current Drug Delivery Even More Complex…. When Mental Disorder Meets Addiction in Youth: Dual Pathology
Current Drug Research Reviews Transcriptional Regulation of CYP2C19 and its Role in Altered Enzyme Activity
Current Drug Metabolism Meet Our Editorial Board Member
Current Neuropharmacology Neuroinflammation, Oxidative Stress and the Pathogenesis of Alzheimers Disease
Current Pharmaceutical Design Discovery of Notch-Sparing γ-Secretase Inhibitors
Current Alzheimer Research Mitochondrial Dysfunction in the Pathophysiology of Bipolar Disorder: Effects of Pharmacotherapy
Mini-Reviews in Medicinal Chemistry Alzheimers Disease (AD) and Mild Cognitive Impairment (MCI) Patients are Characterized by Increased BDNF Serum Levels
Current Alzheimer Research Bacteriophage - A Common Divergent Therapeutic Approach for Alzheimer's Disease and Type II Diabetes Mellitus
CNS & Neurological Disorders - Drug Targets Pharmacological Interventions and Rehabilitation Approach for Enhancing Brain Self-repair and Stroke Recovery
Current Neuropharmacology Structural Chromosome Abnormalities Associated with Obesity: Report of Four New Subjects and Review of Literature
Current Genomics