Synthesis and effects of pyrazolines and isoxazoles on the phagocytic chemotaxis and release of reactive oxygen species by zymosan stimulated human neutrophils

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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 μM). 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.

Original languageEnglish
Pages (from-to)1091-1098
Number of pages8
JournalMedicinal Chemistry
Volume9
Issue number8
DOIs
Publication statusPublished - 2013

Fingerprint

Isoxazoles
Zymosan
Chemotaxis
Inhibitory Concentration 50
Reactive Oxygen Species
Neutrophils
Phagocytes
Luminescence
Luminol
Aptitude
Respiratory Burst
Ibuprofen
Innate Immunity
Human Activities
Aspirin

Keywords

  • Chemiluminescence
  • Chemotactic activity
  • Immunomodulatory
  • Isoxazoles
  • Pyrazolines

ASJC Scopus subject areas

  • Drug Discovery
  • Medicine(all)

Cite this

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title = "Synthesis and effects of pyrazolines and isoxazoles on the phagocytic chemotaxis and release of reactive oxygen species by zymosan stimulated human neutrophils",
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 μM). 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",
author = "{Syed Nasir Abbas}, Bukhari and Ibrahim Jantan and Lam, {Kok Wai} and Lajis, {Nordin Haji} and Faridah Abbas and Malina Jasamai",
year = "2013",
doi = "10.2174/1573406411309080011",
language = "English",
volume = "9",
pages = "1091--1098",
journal = "Medicinal Chemistry",
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TY - JOUR

T1 - Synthesis and effects of pyrazolines and isoxazoles on the phagocytic chemotaxis and release of reactive oxygen species by zymosan stimulated human neutrophils

AU - Syed Nasir Abbas, Bukhari

AU - Jantan, Ibrahim

AU - Lam, Kok Wai

AU - Lajis, Nordin Haji

AU - Abbas, Faridah

AU - Jasamai, Malina

PY - 2013

Y1 - 2013

N2 - 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 μM). 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.

AB - 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 μM). 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.

KW - Chemiluminescence

KW - Chemotactic activity

KW - Immunomodulatory

KW - Isoxazoles

KW - Pyrazolines

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