Abstract
Various 6-phenyl-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazine derivatives (3a-3n) were designed keeping in view the wide bioactivities of 1,2,4-triazoles and their fused heterocyclic derivatives. All target compounds 3a-3n, characterized by IR, 1H-NMR and MS, have been evaluated for their anticonvulsant activity against MES-induced seizures. The pharmacological results showed that most of the compounds displayed some degree of anticonvulsant activity. Among them, 6-(4-chlorophenyl)-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazine (3h) was the most promising compound with an ED50 value of 40.9 mg/kg and a PI value of 6.5.
Keywords: Anticonvulsant, 1,2,4-Triazole, [1,3,4]Thiadiazine, Maximal electroshock test, Neurotoxicity, triazoles, epilepsy, antimicrobial, anticancer, nucleophilic centers, N-bridged heterocycles, phenacyl bromides, H-NMR, pharmacological testing, Elemental analyses
Letters in Drug Design & Discovery
Title: Synthesis and Anticonvulsant Activity Evaluation of 6-phenyl-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazines
Volume: 8 Issue: 8
Author(s): Ming-Xia Song, Chun-Bo Zhang, Xian-Qing Deng, Zhi-Gang Sun and Zhe-Shan Quan
Affiliation:
Keywords: Anticonvulsant, 1,2,4-Triazole, [1,3,4]Thiadiazine, Maximal electroshock test, Neurotoxicity, triazoles, epilepsy, antimicrobial, anticancer, nucleophilic centers, N-bridged heterocycles, phenacyl bromides, H-NMR, pharmacological testing, Elemental analyses
Abstract: Various 6-phenyl-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazine derivatives (3a-3n) were designed keeping in view the wide bioactivities of 1,2,4-triazoles and their fused heterocyclic derivatives. All target compounds 3a-3n, characterized by IR, 1H-NMR and MS, have been evaluated for their anticonvulsant activity against MES-induced seizures. The pharmacological results showed that most of the compounds displayed some degree of anticonvulsant activity. Among them, 6-(4-chlorophenyl)-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazine (3h) was the most promising compound with an ED50 value of 40.9 mg/kg and a PI value of 6.5.
Export Options
About this article
Cite this article as:
Song Ming-Xia, Zhang Chun-Bo, Deng Xian-Qing, Sun Zhi-Gang and Quan Zhe-Shan, Synthesis and Anticonvulsant Activity Evaluation of 6-phenyl-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazines, Letters in Drug Design & Discovery 2011; 8 (8) . https://dx.doi.org/10.2174/157018011796575962
DOI https://dx.doi.org/10.2174/157018011796575962 |
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
-
PET Radioligands for In Vivo Visualization of Neuroinflammation
Current Pharmaceutical Design Children with Medical Complexity: Forwarding a Policy Agenda
Current Pediatric Reviews Status Epilepticus in the Immature Rodent Brain Alters the Dynamics of Autophagy
Current Neurovascular Research Graphical Abstracts:
Central Nervous System Agents in Medicinal Chemistry A Key Role for Connexin Hemichannels in Spreading Ischemic Brain Injury
Current Drug Targets A Review of the Diagnostic Scope of Biomarker Techniques, Genetic Screening and Virtual Scanning
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) Structural MRI Biomarkers of Mild Cognitive Impairment from Young Elders to Centenarians
Current Alzheimer Research Pathophysiology of Transmissible Spongiform Encephalopathies
Current Medicinal Chemistry - Immunology, Endocrine & Metabolic Agents Tau, Amyloid Beta and Deep Brain Stimulation: Aiming to Restore Cognitive Deficit in Alzheimer's Disease
Current Alzheimer Research The Impact of Combination Therapy with a-Blockers and 5ARIs on the Progression of BPH
Current Drug Targets Heat Shock Proteins and Ion Channels. Functional Interactions and Therapeutic Consequences
Current Pharmaceutical Biotechnology Ion Channels as Medicinal Targets of Biological Toxins: The Impact of Automated Patch-Clamp Electrophysiology
Current Topics in Medicinal Chemistry Current and Future Prospective of a Versatile Moiety: Imidazole
Current Drug Targets A Systematic Review of Plant-Derived Natural Compounds for Anxiety Disorders
Current Topics in Medicinal Chemistry Advances in Neuroimaging for HIV-1 Associated Neurological Dysfunction: Clues to the Diagnosis, Pathogenesis and Therapeutic Monitoring
Current HIV Research Neurological Complications of Anderson-Fabry Disease
Current Pharmaceutical Design Importance of P-gp PET Imaging in Pharmacology
Current Pharmaceutical Design Transitional Polytherapy: Tricks of the Trade for Monotherapy to Monotherapy AED Conversions
Current Neuropharmacology The Protective Effects of Natural Products on Blood-Brain Barrier Breakdown
Current Medicinal Chemistry Whole Embryo Culture: An Important Tool in Developmental Toxicology Today
Current Pharmaceutical Design