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 |
- 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
-
Natural Anticancer Agents: Their Therapeutic Potential, Challenges
and Promising Outcomes
Current Medicinal Chemistry HuR as Therapeutic Target in Cancer: What the Future Holds
Current Medicinal Chemistry Silymarin as a New Hepatoprotective Agent in Experimental Cholestasis: New Possibilities for an Ancient Medication
Current Medicinal Chemistry The Anti-inflammatory Potential of the Filarial Nematode Secreted Product, ES-62
Current Topics in Medicinal Chemistry On Mechanisms of Reactive Metabolite Formation from Drugs
Mini-Reviews in Medicinal Chemistry Promising Anti-Fibrotic Approaches for Future Treatment of Systemic Sclerosis
Current Rheumatology Reviews Kruppel-Like Factor 2 (KLF2) Regulates Monocyte Differentiation and Functions in mBSA and IL-1β-Induced Arthritis
Current Molecular Medicine Peripheral and Central Mechanisms of Mechanical Allodynia: Neurokinin Receptor for Therapeutic Target
Central Nervous System Agents in Medicinal Chemistry Therapeutic Potential of Plant Metabolites in Bone Apoptosis: A Review
Current Drug Targets Validation of the Neuroinflammation Cycle as a Drug Discovery Target Using Integrative Chemical Biology and Lead Compound Development with an Alzheimers Disease-Related Mouse Model
Current Alzheimer Research Hypertension Impairs Cerebral Blood Flow in a Mouse Model for Alzheimer’s Disease
Current Alzheimer Research Electrotransfer into Skeletal Muscle for Protein Expression
Current Gene Therapy Significance of Pharmacogenetics and Pharmacogenomics Research in Current Medical Practice
Current Drug Metabolism Morin Inhibits Ovarian Cancer Growth through the Inhibition of NF-κB Signaling Pathway
Anti-Cancer Agents in Medicinal Chemistry Bioinformatics-based Identification of Proteins Expressed by Arthropod- borne Viruses Transmitted by <i>Aedes Aegypti</i> Mosquito
Current Proteomics Antiviral Agents for Influenza: Molecular Targets, Concerns of Resistance, and New Treatment Options
Current Drug Targets Involvement of Rat Hippocampal Astrocytes in β-Amyloid-Induced Angiogenesis and Neuroinflammation
Current Alzheimer Research Diagnosis and Treatment of Alzheimers Disease
Current Medicinal Chemistry - Central Nervous System Agents Delineating Somatostatins Neuronal Actions
Current Drug Targets - CNS & Neurological Disorders Adenosine and Adenosine Receptors in the Pathomechanism and Treatment of Respiratory Diseases
Current Medicinal Chemistry