Abstract
A series of cinnamylpiperazine derivatives was synthesized using different benzophenone as starting material. The structures of the compounds were proved by their IR, 1H-NMR spectroscopic data and mass spectra data. The anticonvulsant activities of these compounds were evaluated with maximal electroshock (MES) test and rotarod test with intraperitoneal injection on KunMing mice. Among all the flunarizine analogues, no one exhibited better anticonvulsant activity than flunarizine. Flunarizine (4i) exhibited anticonvulsant activity with ED50 of 38.1 mg/kg, TD50 of 164.3 mg/kg and PI of 4.3 through administration intraperitoneal, and with ED50 of 56.8 mg/kg, TD50 of 456.3 mg/kg and PI of 8.0 through oral administration.
Keywords: Anticonvulsant, MES, Calcium channel, Flunarizine, Cinnarizine, Cinnamyl piperazine, Anticonvulsant activity, Cinnamylpiperazine Derivatives, Refractory childhood epilepsy, Structure activity relationship, Program (ADD), Drug Development, Intrinsic burst firing, Excitotoxic, Apoptotic cell, Pharmacology, Tonic maximal extension, Rotarod Test, Cinnarizine-induced parkinsonism
Letters in Drug Design & Discovery
Title: Synthesis and Anticonvulsant Activity of Some Cinnamylpiperazine Derivatives
Volume: 7 Issue: 9
Author(s): Chuan Hu, Zhi-Gang Sun, Cheng-Xi Wei and Zhe-Shan Quan
Affiliation:
Keywords: Anticonvulsant, MES, Calcium channel, Flunarizine, Cinnarizine, Cinnamyl piperazine, Anticonvulsant activity, Cinnamylpiperazine Derivatives, Refractory childhood epilepsy, Structure activity relationship, Program (ADD), Drug Development, Intrinsic burst firing, Excitotoxic, Apoptotic cell, Pharmacology, Tonic maximal extension, Rotarod Test, Cinnarizine-induced parkinsonism
Abstract: A series of cinnamylpiperazine derivatives was synthesized using different benzophenone as starting material. The structures of the compounds were proved by their IR, 1H-NMR spectroscopic data and mass spectra data. The anticonvulsant activities of these compounds were evaluated with maximal electroshock (MES) test and rotarod test with intraperitoneal injection on KunMing mice. Among all the flunarizine analogues, no one exhibited better anticonvulsant activity than flunarizine. Flunarizine (4i) exhibited anticonvulsant activity with ED50 of 38.1 mg/kg, TD50 of 164.3 mg/kg and PI of 4.3 through administration intraperitoneal, and with ED50 of 56.8 mg/kg, TD50 of 456.3 mg/kg and PI of 8.0 through oral administration.
Export Options
About this article
Cite this article as:
Hu Chuan, Sun Zhi-Gang, Wei Cheng-Xi and Quan Zhe-Shan, Synthesis and Anticonvulsant Activity of Some Cinnamylpiperazine Derivatives, Letters in Drug Design & Discovery 2010; 7 (9) . https://dx.doi.org/10.2174/157018010792929595
DOI https://dx.doi.org/10.2174/157018010792929595 |
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
-
Conotoxin Superfamily Prediction Using Diffusion Maps Dimensionality Reduction and Subspace Classifier
Current Protein & Peptide Science Editorial [Hot Topic: Calcium Regulatory Proteins as Therapeutic Targets (Guest Editor: Livia C. Hool)]
Current Drug Targets The Use of Microarrays to Study Childhood Developmental Brain Disorders
Current Genomics Editorial:Cannabis: Neurological Correlates in Abuse and Medical Use
CNS & Neurological Disorders - Drug Targets Human Disease and Drug Pharmacology, Complex as Real Life
Current Medicinal Chemistry Attempted Cell Cycle Induction in Post-Mitotic Neurons Occurs in Early and Late Apoptotic Programs Through Rb, E2F1, and Caspase 3
Current Neurovascular Research Neuropeptides and Other Chemical Mediators, and the Role of Anti-inflammatory Drugs in Primary Headaches
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Microemulsions as Carriers for Therapeutic Molecules
Recent Patents on Drug Delivery & Formulation AMPA Receptor Antagonists: Potential Therapeutic Applications
Recent Patents on CNS Drug Discovery (Discontinued) Enantiopure 1,2,3-Triazolyl-β-amino Acids via Click Cycloaddition Reaction on Racemic Alkynyl Precursors Followed by Separation of Stereoisomers
Current Topics in Medicinal Chemistry GABA-A Receptor Complex and Memory Processes
Medicinal Chemistry Reviews - Online (Discontinued) Patent Selections:
Recent Patents on CNS Drug Discovery (Discontinued) Neuropeptides as Therapeutic Targets to Combat Stress-Associated Behavioral and Neuroendocrinological Effects
CNS & Neurological Disorders - Drug Targets Editorial
Current Medicinal Chemistry Regulation of Self-Reactive T Cells by Human Immunoglobulins- Implications for Multiple Sclerosis Therapy
Current Pharmaceutical Design “Epileptic Encephalopathy” of Infancy and Childhood: Electro-Clinical Pictures and Recent Understandings
Current Neuropharmacology Gold and Silver Nanoparticles for Applications in Theranostics
Current Topics in Medicinal Chemistry Insulin Resistance as Common Molecular Denominator Linking Obesity to Alzheimer’s Disease
Current Alzheimer Research PDZ Domain Protein-Protein Interactions: A Case Study with PICK1
Current Topics in Medicinal Chemistry Strategies for Strengthening Patent Protection of Pharmaceutical Inventions in Light of Federal Court Decisions
Current Topics in Medicinal Chemistry