Abstract
We have evaluated as sodium channel blockers a series of imidazobenzoxazines, imidazobenzoxazin-5-ones and imidazobenzoxazin-5-thiones. We tested these new compounds on NaV1.6 and NaV1.2 sodium channel isoforms, that are expressed in central nervous system and seems to be very important in controlling neuronal firing. Moreover, mutations in SCN2A, the gene encoding NaV1.2, have been identified in patients with generalized epilepsy. Almost all of the new molecules were able to block the NaV1.6 sodium currents and some of them displayed IC50 values in the low micromolar range.
Keywords: Antiepileptic drugs, Imidazobenzoxazines, NaV1.6 sodium channel isoforms, Voltage gated sodium channels.
Letters in Drug Design & Discovery
Title:Biological Evaluation of Imidazobenzoxazines, Imidazobenzoxazin-5-ones and Imidazobenzoxazin-5-thiones as Sodium Channel Blockers
Volume: 11 Issue: 1
Author(s): Mirko Rivara, Valentina Zuliani and Manoj K. Patel
Affiliation:
Keywords: Antiepileptic drugs, Imidazobenzoxazines, NaV1.6 sodium channel isoforms, Voltage gated sodium channels.
Abstract: We have evaluated as sodium channel blockers a series of imidazobenzoxazines, imidazobenzoxazin-5-ones and imidazobenzoxazin-5-thiones. We tested these new compounds on NaV1.6 and NaV1.2 sodium channel isoforms, that are expressed in central nervous system and seems to be very important in controlling neuronal firing. Moreover, mutations in SCN2A, the gene encoding NaV1.2, have been identified in patients with generalized epilepsy. Almost all of the new molecules were able to block the NaV1.6 sodium currents and some of them displayed IC50 values in the low micromolar range.
Export Options
About this article
Cite this article as:
Rivara Mirko, Zuliani Valentina and Patel K. Manoj, Biological Evaluation of Imidazobenzoxazines, Imidazobenzoxazin-5-ones and Imidazobenzoxazin-5-thiones as Sodium Channel Blockers, Letters in Drug Design & Discovery 2014; 11 (1) . https://dx.doi.org/10.2174/15701808113109990050
DOI https://dx.doi.org/10.2174/15701808113109990050 |
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
-
Effects of Low Doses of Polyunsaturated Fatty Acids on the Attention Deficit/Hyperactivity Disorder of Children: A Systematic Review
Current Neuropharmacology Possible Protecting Role of TNF-α in Kainic Acid-induced Neurotoxicity Via Down-Regulation of NFκB Signaling Pathway
Current Alzheimer Research Editorial:Cannabis: Neurological Correlates in Abuse and Medical Use
CNS & Neurological Disorders - Drug Targets Editorial [Pharmacology and Therapeutic Activity of Purinergic Drugs for Disorders of the Nervous System]
CNS & Neurological Disorders - Drug Targets Shining Light on an mGlu5 Photoswitchable NAM: A Theoretical Perspective
Current Neuropharmacology Effects of Static Magnetic Fields on Blood Pressure in Animals and Humans
Current Hypertension Reviews Ultrasonic Assisted Synthesis, Biological Evaluation, and Molecular Docking of Chalcone-based 1,5-benzodiazepine as Potential Anticonvulsant Agents
Current Enzyme Inhibition Current Status of Complementary and Alternative Medicine in the Treatment of Rheumatic Disease Pain
Current Rheumatology Reviews Viral M2 Ion Channel Protein: A Promising Target for Anti-influenza Drug Discovery
Mini-Reviews in Medicinal Chemistry Integration of Pharmacogenomics and Pharmacometrics to Support Drug Development, Regulatory and Therapeutic Decisions
Current Pharmacogenomics and Personalized Medicine Comparison of Valvulopathy Risk with Lorcaserin and Phenterminetopiramate for Weight Loss
Current Drug Therapy Pharmacoproteomics Applications for Drug Target Discovery in CNS Disorders
Current Pharmacogenomics and Personalized Medicine Combating Diseases with Computational Strategies Used for Drug Design and Discovery
Current Topics in Medicinal Chemistry Nutrition and Bone Health: Its Relationship to Osteoporosis
Current Nutrition & Food Science History Repeats Itself: Pharmacodynamic Trends in the Treatment of Anxiety Disorders
Current Pharmaceutical Design Immunoproteasome in Cancer and Neuropathologies: A New Therapeutic Target?
Current Pharmaceutical Design Relevance of Follow-Up in Patients with Core Clinical Criteria for Alzheimer Disease and Normal CSF Biomarkers
Current Alzheimer Research The GABAergic System and the Gastrointestinal Physiopathology
Current Pharmaceutical Design Ionotropic Glutamate Receptors & CNS Disorders
CNS & Neurological Disorders - Drug Targets Strategies to Improve the Killing of Tumors Using Temozolomide: Targeting the DNA Repair Protein MGMT
Current Medicinal Chemistry