Abstract
Local anesthetics are the most widely consumed drugs in the practice of medicine which provide a loss of sensation in a certain body part without loss of consciousness or impairment of central control of essential functions. Lidocaine (I) is the most commonly local anaesthetic drug which is widely used in all species due to its fabulous diffusing and penetrating properties as well as prompt onset of surgical analgesia. In this study, new aminobenzothiazole (with many useful biological and pharmacological properties) analogues were synthesized by changing of amine moiety of I. Both acute and chronic pain properties of new compounds (II-VI) were studied by using the tail immersion and formalin tests on mice and the outcomes were compared with control and lidocaine groups. According to the results, aminobenzothiazole derivatives are better candidates than diethylamine group for replacement on amine moiety of I. Also, derivatives with electron-withdrawing groups on this amine (V and VI) could decrease pain better than electron-donating ones (II and III) (specially on position 6 of this amine, II and V) which may be of concern for blockade of specific sodium channels by these new compounds.
Keywords: Lidocaine, local anesthetics, aminobenzothiazole, acute and chronic pains, tail immersion and formalin tests.
Combinatorial Chemistry & High Throughput Screening
Title:Synthesis and Analgesic Properties of Lidocaine Derivatives with Substituted Aminobenzothiazoles
Volume: 19 Issue: 6
Author(s): Abbas Ahmadi, Mohsen Khalili, Mohammad Kazem Mohammadinoude and Babak Nahri-Niknafs
Affiliation:
Keywords: Lidocaine, local anesthetics, aminobenzothiazole, acute and chronic pains, tail immersion and formalin tests.
Abstract: Local anesthetics are the most widely consumed drugs in the practice of medicine which provide a loss of sensation in a certain body part without loss of consciousness or impairment of central control of essential functions. Lidocaine (I) is the most commonly local anaesthetic drug which is widely used in all species due to its fabulous diffusing and penetrating properties as well as prompt onset of surgical analgesia. In this study, new aminobenzothiazole (with many useful biological and pharmacological properties) analogues were synthesized by changing of amine moiety of I. Both acute and chronic pain properties of new compounds (II-VI) were studied by using the tail immersion and formalin tests on mice and the outcomes were compared with control and lidocaine groups. According to the results, aminobenzothiazole derivatives are better candidates than diethylamine group for replacement on amine moiety of I. Also, derivatives with electron-withdrawing groups on this amine (V and VI) could decrease pain better than electron-donating ones (II and III) (specially on position 6 of this amine, II and V) which may be of concern for blockade of specific sodium channels by these new compounds.
Export Options
About this article
Cite this article as:
Ahmadi Abbas, Khalili Mohsen, Kazem Mohammadinoude Mohammad and Nahri-Niknafs Babak, Synthesis and Analgesic Properties of Lidocaine Derivatives with Substituted Aminobenzothiazoles, Combinatorial Chemistry & High Throughput Screening 2016; 19 (6) . https://dx.doi.org/10.2174/1386207319666160517115310
DOI https://dx.doi.org/10.2174/1386207319666160517115310 |
Print ISSN 1386-2073 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5402 |
Call for Papers in Thematic Issues
Artificial Intelligence Methods for Biomedical, Biochemical and Bioinformatics Problems
Recently, a large number of technologies based on artificial intelligence have been developed and applied to solve a diverse range of problems in the areas of biomedical, biochemical and bioinformatics problems. By utilizing powerful computing resources and massive amounts of data, methods based on artificial intelligence can significantly improve the ...read more
Eco-friendly Agents for Biological Control of Pathogenic Diseases
The discovery of an alternative biological approach to disease management includes work on medicinal products derived from natural sources as a starting point for the development of eco-friendly agents for these diseases and the injuries they cause, as well as reducing human contact with hazardous chemicals and their residues. We ...read more
Emerging trends in diseases mechanisms, noble drug targets and therapeutic strategies: focus on immunological and inflammatory disorders
Recently infectious and inflammatory diseases have been a key concern worldwide due to tremendous morbidity and mortality world Wide. Recent, nCOVID-9 pandemic is a good example for the emerging infectious disease outbreak. The world is facing many emerging and re-emerging diseases out breaks at present however, there is huge lack ...read more
Exploring Spectral Graph Theory in Combinatorial Chemistry
Scope of the Thematic Issue: Combinatorial chemistry involves the synthesis and analysis of a large number of diverse compounds simultaneously. Traditional methods rely on brute force experimentation, which can be time-consuming and resource-intensive. Spectral Graph Theory, a branch of mathematics dealing with the properties of graphs in relation to the ...read more
- 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
-
Synthetic Cannabinoids: Psychopharmacology, Clinical Aspects, Psychotic Onset
CNS & Neurological Disorders - Drug Targets Effects of Opiates and HIV Proteins on Neurons: The Role of Ferritin Heavy Chain and a Potential for Synergism
Current HIV Research An Efficient Cancer Classification Model for CT/MRI/PET Fused Images
Current Medical Imaging Targeting Pain-evoking Transient Receptor Potential Channels for the Treatment of Pain
Current Neuropharmacology Transport of Bupropion and its Metabolites by the Model CHO and HEK293 Cell Lines
Drug Metabolism Letters Nucleic Acids as Targets for Antitelomerase Agents
Mini-Reviews in Medicinal Chemistry The Sphingolipid Rheostat: A Potential Target for Improving Pancreatic Islet Survival and Function
Endocrine, Metabolic & Immune Disorders - Drug Targets Structural Neuroimaging Findings in Major Depressive Disorder Throughout Aging: A Critical Systematic Review of Prospective Studies
CNS & Neurological Disorders - Drug Targets Antioxidant Properties of Nitric Oxide in Cellular Physiological and Pathophysiological Mechanisms. The Implications of Biological Balance between NO and Oxidative Stress
Current Medicinal Chemistry - Anti-Inflammatory & Anti-Allergy Agents SELDI Protein Chip Technology for the Detection of Serum Biomarkers for Liver Disease
Protein & Peptide Letters Patent Selections
Recent Patents on Inflammation & Allergy Drug Discovery Study of the Relationships between COVID-19, Associated Diseases, and Vitamins
Coronaviruses Italian Association of Clinical Endocrinologists (AME) and Italian AACE Chapter Position Statement for Clinical Practice: Assessment of Response to Treatment and Follow-Up in Gastroenteropancreatic Neuroendocrine Neoplasms
Endocrine, Metabolic & Immune Disorders - Drug Targets The Influence of Ca<sup>2+</sup> and Zn<sup>2+</sup> on the Amyloid Fibril Formation by β-Casein
Protein & Peptide Letters Pharmaceutical Nanotechnology United States Patent Watch (October – December 2014)
Pharmaceutical Nanotechnology Editorial [Hot Topic: Applications of Angiotensin Converting Enzyme Inhibitors and of Angiotensin II Receptor Blockers in Pharmacology and Therapy: An Update (Executive Editor: Agostino Molteni)]
Current Pharmaceutical Design Functional Selectivity in Cannabinoid Signaling
Current Molecular Pharmacology Inhibition of β-Amyloid Aggregation by Albiflorin, Aloeemodin and Neohesperidin and their Neuroprotective Effect on Primary Hippocampal Cells Against β-Amyloid Induced Toxicity
Current Alzheimer Research Molecule of the Month
Current Topics in Medicinal Chemistry Development of New Drugs that Act Through Membrane Receptors and Involve an Action of Inverse Agonism
Recent Patents on CNS Drug Discovery (Discontinued)