Synthesis and Effects of Pyrazolines and Isoxazoles on the Phagocytic Chemotaxis and Release of Reactive Oxygen Species by Zymosan Stimulated Human Neutrophils

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.

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