Abstract
A series of novel isoxazole and pyrazoline derivatives has been synthesized and evaluated for their effects on the chemiluminescence and chemotactic activity of human phagocytes. Their effects on the chemotactic migration of isolated polymorphonuclear leukocytes (PMNs) and on the release of reactive oxygen species (ROS) during respiratory burst of human whole blood and PMNs were carried out using the Boyden chamber technique and luminol-based chemiluminescence assay, respectively. Of the compounds tested, compounds 8, 9, 11 and 12 exhibited higher inhibitory activity on the release of ROS (with IC50 values ranging from 5.6 to 8.4 μM) than acetylsalicylic acid (IC50 = 9.5 μ M). These compounds also showed strong inhibitory activity on the migration of PMNs with compound 8 exhibiting an IC50 value lower than that of ibuprofen. The results suggest that some of these isoxazole and pyrazoline derivatives have ability to modulate the innate immune response of phagocytes at different steps, indicating their potential as a source of new immunomodulatory agents.
Keywords: Chemiluminescence, chemotactic activity, immunomodulatory, isoxazoles, pyrazolines.
Medicinal Chemistry
Title:Synthesis and Effects of Pyrazolines and Isoxazoles on the Phagocytic Chemotaxis and Release of Reactive Oxygen Species by Zymosan Stimulated Human Neutrophils
Volume: 9 Issue: 8
Author(s): Syed Nasir Abbas Bukhari, Ibrahim Jantan, Lam Kok Wai, Nordin Haji Lajis, Faridah Abbas and Malina Jasamai
Affiliation:
Keywords: Chemiluminescence, chemotactic activity, immunomodulatory, isoxazoles, pyrazolines.
Abstract: A series of novel isoxazole and pyrazoline derivatives has been synthesized and evaluated for their effects on the chemiluminescence and chemotactic activity of human phagocytes. Their effects on the chemotactic migration of isolated polymorphonuclear leukocytes (PMNs) and on the release of reactive oxygen species (ROS) during respiratory burst of human whole blood and PMNs were carried out using the Boyden chamber technique and luminol-based chemiluminescence assay, respectively. Of the compounds tested, compounds 8, 9, 11 and 12 exhibited higher inhibitory activity on the release of ROS (with IC50 values ranging from 5.6 to 8.4 μM) than acetylsalicylic acid (IC50 = 9.5 μ M). These compounds also showed strong inhibitory activity on the migration of PMNs with compound 8 exhibiting an IC50 value lower than that of ibuprofen. The results suggest that some of these isoxazole and pyrazoline derivatives have ability to modulate the innate immune response of phagocytes at different steps, indicating their potential as a source of new immunomodulatory agents.
Export Options
About this article
Cite this article as:
Abbas Bukhari Nasir Syed, Jantan Ibrahim, Wai Kok Lam, Lajis Haji Nordin, Abbas Faridah and Jasamai Malina, Synthesis and Effects of Pyrazolines and Isoxazoles on the Phagocytic Chemotaxis and Release of Reactive Oxygen Species by Zymosan Stimulated Human Neutrophils, Medicinal Chemistry 2013; 9 (8) . https://dx.doi.org/10.2174/1573406411309080011
DOI https://dx.doi.org/10.2174/1573406411309080011 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
Call for Papers in Thematic Issues
Carbohydrates in Computational and Medicinal Chemistry
Carbohydrates are the most essential organic molecules and are involved in the maintenance of various physiological and metabolic processes in living organisms. Carbohydrate-based compounds have come to the attention of researchers because of their significant contributions to biological functions, such as cell development and cell proliferation, connections between several cells, ...read more
Recent Advances in the Medicinal Chemistry of Cancer
Scope of the Thematic Issue: Correlation between structure and function is one of the important aspects of the success of anti-cancer compounds associated with their structure-activity interactions, physiology, biochemical, molecular, and genetic processes. Overcoming these obstacles is key to obtaining further insights into developments in rational drug design, bioorganic chemistry, ...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
-
New Targets, New Hope: Novel Drug Targets for Curbing Malaria
Mini-Reviews in Medicinal Chemistry Recent Developments of Amidine-like Compounds as Selective NOS Inhibitors
Current Enzyme Inhibition ACAT1 as a Therapeutic Target and its Genetic Relationship with Alzheimer's Disease
Current Alzheimer Research Hepatic Mediators of Lipid Metabolism and Ketogenesis: Focus on Fatty Liver and Diabetes
Current Diabetes Reviews The Histone Deacetylase SIRT6: At the Crossroads Between Epigenetics, Metabolism and Disease
Current Topics in Medicinal Chemistry Role of Estrogen Receptors and GPR30/GPER in Glucose Homeostasis
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) Regulation of Protective and Pathogenic Th17 Responses
Current Immunology Reviews (Discontinued) Pertinence of Apoptosis Markers for the Improvement of In Vitro Fertilization (IVF)
Current Medicinal Chemistry AAV-mediated Overexpression of IL-10 Mitigates the Inflammatory Cascade in Stimulated Equine Chondrocyte Pellets
Current Gene Therapy Mechanisms of Viral Hepatitis Induced Liver Injury
Current Molecular Medicine Histamine H4 Receptor: A Novel Therapeutic Target for Immune and Allergic Responses
Mini-Reviews in Medicinal Chemistry Role of Microglia in Psychostimulant Addiction
Current Neuropharmacology Recent Advances in Pharmacological Interventions of Chronic Prostatitis/ Chronic Pelvic Pain Syndrome
Current Pharmaceutical Design CellSaic, A Cell Aggregate-Like Technology Using Recombinant Peptide Pieces for MSC Transplantation
Current Stem Cell Research & Therapy JAK Inhibition as a Therapeutic Strategy for Inflammatory Bowel Disease
Current Drug Metabolism Diagnostics and Therapy of Antineutrophil Cytoplasmic Antibody (ANCA) Associated Vasculitides
Current Pharmaceutical Design Integrins and Cancer: Gene Expression, Epigenetics and Metastasis
Current Genomics Future Perspectives in the Pharmacological Treatment of Atrial Fibrillation and Ventricular Arrhythmias in Heart Failure
Current Pharmaceutical Design Evaluation of Different Signal Peptides for Secretory Production of Recombinant Human Interferon-gamma: Bioinformatics Approach
Letters in Drug Design & Discovery Antiviral Agents for Influenza: Molecular Targets, Concerns of Resistance, and New Treatment Options
Current Drug Targets