Abstract
A series of new 2,5-disubstituted-1,3,4-oxadiazole derivatives 8(a-o) was synthesized by the reaction of 1-(5- phenyl-1,3,4-oxadiazol-2-yl)piperazine with various sulfonyl chlorides. The synthesized compounds were characterized by elemental analyses, 1H NMR, 13C NMR and mass spectral studies. The newly synthesized compounds were screened for their anticonvulsant activity against maximal electroshock (MES) seizure method and compared with the standard drug phenytoin. The neurotoxic effects were determined by rotorod test. Compounds 8d, 8e and 8f were found to be most potent of this series. The same compounds showed no neurotoxicity at the maximum dose administered (100 mg/kg). The efforts were also made to establish the structure activity relationships among synthesized compounds.
Keywords: Synthesis, 1, 3, 4-oxadiazole, Anticonvulsant activity, Neurotoxicity, Rotorod.
Letters in Drug Design & Discovery
Title:Synthesis and Evaluation of In Vivo Anticonvulsant Activity of 2,5- Disubstituted-1,3,4-Oxadiazole Derivatives
Volume: 10 Issue: 8
Author(s): Kikkeri P. Harish, Kikkeri N. Mohana, Lingappa Mallesha, B. Veeresh, B. Madhava Reddy and Nagula Naresh Kumar
Affiliation:
Keywords: Synthesis, 1, 3, 4-oxadiazole, Anticonvulsant activity, Neurotoxicity, Rotorod.
Abstract: A series of new 2,5-disubstituted-1,3,4-oxadiazole derivatives 8(a-o) was synthesized by the reaction of 1-(5- phenyl-1,3,4-oxadiazol-2-yl)piperazine with various sulfonyl chlorides. The synthesized compounds were characterized by elemental analyses, 1H NMR, 13C NMR and mass spectral studies. The newly synthesized compounds were screened for their anticonvulsant activity against maximal electroshock (MES) seizure method and compared with the standard drug phenytoin. The neurotoxic effects were determined by rotorod test. Compounds 8d, 8e and 8f were found to be most potent of this series. The same compounds showed no neurotoxicity at the maximum dose administered (100 mg/kg). The efforts were also made to establish the structure activity relationships among synthesized compounds.
Export Options
About this article
Cite this article as:
Harish P. Kikkeri, Mohana N. Kikkeri, Mallesha Lingappa, Veeresh B., Reddy Madhava B. and Kumar Naresh Nagula, Synthesis and Evaluation of In Vivo Anticonvulsant Activity of 2,5- Disubstituted-1,3,4-Oxadiazole Derivatives, Letters in Drug Design & Discovery 2013; 10 (8) . https://dx.doi.org/10.2174/15701808113109990020
DOI https://dx.doi.org/10.2174/15701808113109990020 |
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
-
Nanoemulgel: A Promising Phase in Drug Delivery
Current Pharmaceutical Design A Focus on Microfluidics and Nanotechnology Approaches for the Ultra Sensitive Detection of MicroRNA
MicroRNA Metabolic Basis of Sporadic Alzeimer’s Disease. Role of Hormones Related to Energy Metabolism
Current Pharmaceutical Design Recent Multiple Transition Metal Catalysed Single-Pot Reactions
Current Organic Synthesis Clinical Profile of Mortality among Chronic Schizophrenic Patients: A Local Pilot Survey in Iran
Current Psychiatry Research and Reviews The Role of P-Glycoprotein in Psychiatric Disorders: A Reliable Guard of the Brain?
Central Nervous System Agents in Medicinal Chemistry Comprehensive Assessment of ADMET Risks in Drug Discovery
Current Pharmaceutical Design Synthesis and Anticonvulsant Activity Evaluation of Some 1-alkoxy-4-(1H- 1,2,4-triazol-1-yl)phthalazines
Letters in Drug Design & Discovery Exploring the Role of “Brahmi” (Bacopa monnieri and Centella asiatica) in Brain Function and Therapy
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery An Overview of HDAC Inhibitors and their Synthetic Routes
Current Topics in Medicinal Chemistry Transient Receptor Potential Channels - Emerging Novel Drug Targets for the Treatment of Pain
Current Medicinal Chemistry Editorial [Hot topic:VIP and PACAP: Novel Approaches to Brain Functions and Neuroprotection (Executive Guest Editors: Seiji Shioda and Illana Gozes)]
Current Pharmaceutical Design Repetitive Transcranial Magnetic Stimulation to Treat Substance Use Disorders and Compulsive Behavior
CNS & Neurological Disorders - Drug Targets TrkB Receptor Agonist 7, 8 Dihydroxyflavone Triggers Profound Gender- Dependent Neuroprotection in Mice After Perinatal Hypoxia and Ischemia
CNS & Neurological Disorders - Drug Targets Design, Synthesis and in silico Studies of New 5-substituted-2-(2-(5-aryl- 1H-1, 2, 4-triazole-3-ylthio) acetyl) Hydrazine Carbothioamide/ Carboxamides for Anticonvulsant Activity
Letters in Drug Design & Discovery Physiological Effect and Therapeutic Application of Alpha Lipoic Acid
Current Medicinal Chemistry Computational Drug Repositioning: A Lateral Approach to Traditional Drug Discovery?
Current Topics in Medicinal Chemistry GABAergic Modulation in Diabetic Encephalopathy-Related Depression
Current Pharmaceutical Design Antiepileptics and the Treatment of Neuropathic Pain: Evidence from Animal Models
Current Pharmaceutical Design Meet Our Editorial Board Member
Current Neuropharmacology