Abstract
Two series of 1-alkyl-4-(4H-1,2,4-triazol-4-yl)piperidines and 1-alkyl-4-(2H-1,2,4-triazol-3-one-4-yl) piperidines were synthesized and their anticonvulsant and antibacterial activities were evaluated. Pharmacological tests showed that three of the synthesized compounds (6c, 6k, 7m) displayed 100% protection at a dose of 100 mg/kg. 4-(1- Octylpiperidin-4-yl)-2,4-dihydro-3H-1,2,4-triazol-3-one (6c) was the most active compound in this study, with an ED50 of 65.4 mg/kg and a TD50 value of 241.2 mg/kg, resulting in a PI of 3.6. Four of the synthesized compounds showed potent inhibitory activity against gram positive bacteria staphylococcus aureus (RN4220, KCTC 209 and KCTC 503), especially against the strains of multidrug-resistant clinical isolates (MRSA3167/3506 and QRSA3505/3519). Among which compound 1-tetradeyl-4-(4H-1,2,4-triazol-4-yl)piperidine (7f) showed the most potent levels of activity (MIC = 2 µg/mL) against the gram-positive strains.
Keywords: Antibacterial, anticonvulsant, maximal electroshock test, synthesis, triazole, tiazolone.
Letters in Drug Design & Discovery
Title:Synthesis and Studies on Anticonvulsant and Antibacterial Activities of 1- Alkyl-4-(4H-1,2,4-triazol-4-yl)piperidine Derivatives
Volume: 11 Issue: 9
Author(s): Yan-Ping Yuan, Shi-Ben Wang, Guo-Hua Gong and Zhe-Shan Quan
Affiliation:
Keywords: Antibacterial, anticonvulsant, maximal electroshock test, synthesis, triazole, tiazolone.
Abstract: Two series of 1-alkyl-4-(4H-1,2,4-triazol-4-yl)piperidines and 1-alkyl-4-(2H-1,2,4-triazol-3-one-4-yl) piperidines were synthesized and their anticonvulsant and antibacterial activities were evaluated. Pharmacological tests showed that three of the synthesized compounds (6c, 6k, 7m) displayed 100% protection at a dose of 100 mg/kg. 4-(1- Octylpiperidin-4-yl)-2,4-dihydro-3H-1,2,4-triazol-3-one (6c) was the most active compound in this study, with an ED50 of 65.4 mg/kg and a TD50 value of 241.2 mg/kg, resulting in a PI of 3.6. Four of the synthesized compounds showed potent inhibitory activity against gram positive bacteria staphylococcus aureus (RN4220, KCTC 209 and KCTC 503), especially against the strains of multidrug-resistant clinical isolates (MRSA3167/3506 and QRSA3505/3519). Among which compound 1-tetradeyl-4-(4H-1,2,4-triazol-4-yl)piperidine (7f) showed the most potent levels of activity (MIC = 2 µg/mL) against the gram-positive strains.
Export Options
About this article
Cite this article as:
Yuan Yan-Ping, Wang Shi-Ben, Gong Guo-Hua and Quan Zhe-Shan, Synthesis and Studies on Anticonvulsant and Antibacterial Activities of 1- Alkyl-4-(4H-1,2,4-triazol-4-yl)piperidine Derivatives, Letters in Drug Design & Discovery 2014; 11 (9) . https://dx.doi.org/10.2174/1570180811666140623204022
DOI https://dx.doi.org/10.2174/1570180811666140623204022 |
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
-
Predicting Targeted Polypharmacology for Drug Repositioning and Multi- Target Drug Discovery
Current Medicinal Chemistry Melatonin in Autism Spectrum Disorders
Current Clinical Pharmacology Levofloxacin-Induced Delirium in a Patient Suffering from Schizoaffective Disorder and Multiple Sclerosis
Current Drug Safety Neurodegeneration and Neuroprotection in Multiple Sclerosis
Current Pharmaceutical Design Potential Beneficial Effects of Marine Peptide on Human Neuron Health
Current Protein & Peptide Science Psychoemotional Background of Temporomandibular Joint Dysfunction and Possible Drug Therapy
Letters in Drug Design & Discovery Role of Quercetin in the Mitigation of Lindane Induced Toxicity in Terms of Oxidative Responses and Metabolic Status in Mice Brain
Current Bioactive Compounds Astrocyte-Microglia Cooperation in the Expression of a Pro-Inflammatory Phenotype
CNS & Neurological Disorders - Drug Targets Stem Cells: In Sickness and in Health
Current Stem Cell Research & Therapy Amyloid β Oligomers Decrease Hippocampal Spontaneous Network Activity in an Age-Dependent Manner
Current Alzheimer Research Immunomodulatory Effects of Medicinal Plants used for Vitiligo in Traditional Persian Medicine
Current Drug Discovery Technologies IBD Modern Concepts, Nano Drug Delivery and Patents: An Update
Recent Patents on Nanomedicine Rethinking the Excitotoxic Ionic Milieu:The Emerging Role of Zn 2+ in Ischemic Neuronal Injury
Current Molecular Medicine GABAergic Agonists Modulate the Glutamate Release from Frontal Cortex Synaptosomes of Rats with Experimental Autoimmune Encephalomyelitis
Inflammation & Allergy - Drug Targets (Discontinued) Relationship Between Polymerase Gamma (POLG) Polymorphisms and Antiretroviral Therapy-Induced Lipodystrophy in HIV-1 Infected Patients: A Case-Control Study
Current HIV Research Metabolic Basis of Sporadic Alzeimer’s Disease. Role of Hormones Related to Energy Metabolism
Current Pharmaceutical Design N-Valproyl-L-Phenylalanine as New Potential Antiepileptic Drug: Synthesis, Characterization and In Vitro Studies on Stability, Toxicity and Anticonvulsant Efficacy
Medicinal Chemistry Targeting Cancer Stem Cells with Repurposed Drugs to Improve Current Therapies
Recent Patents on Anti-Cancer Drug Discovery Sleep Disorders Research From 1945 to 2020: A Bibliometric Analysis
CNS & Neurological Disorders - Drug Targets Targeting the Expression of Anti-Apoptotic Proteins by Antisense Oligonucleotides
Current Drug Targets