Assessment of pyrazolone derivatives as a new class of cyclooxygenase-2 and aflatoxigenic fungal inhibitors
Year: 2025
Type: article
Abstract: The development of anti-inflammatory compounds is crucial because of the complexity of the wound-healing process associated with bacterial infections. Anti-inflammatory compounds have been rapidly developed for use in biomedical fields. In this study, three new skin fibroblast cell promotors (pyrazolone derivatives) with pyrazolone cores were designed and synthesized to evaluate their inhibitory effects on the cyclooxygenase-2 enzyme. The pyrazolone derivatives were characterized using FTIR, 1 H and 13 C NMR, and DSC . These pyrazolone derivatives exhibited excellent biocompatibility , resulting in significant proliferation of NIH/3 T3 fibroblast cells, as confirmed through fluorescence microscopy in the live-dead cell assay. Moral anti-inflammatory property was verified by the strong interactions between inflammation-responsible enzyme 6-COX and ligands. In vitro anticancer activity assessments revealed that the pyrazolone derivatives did not reduce the viability of breast cancer MDA-MB231 cells as opposed to the control group. Additionally, the pyrazolone derivatives displayed great antibacterial activity against Staphylococcus aureus and Escherichia coli , with a 100 ± 0.1 % inhibitory efficiency for 24 h. Moreover, the pyrazolone derivatives showed good antifungal activity against Aspergillus flavus , effectively inhibiting the secretion of aflatoxins (98 ± 0.1 %). Our results demonstrated that these newly synthesized pyrazolone derivatives are promising candidates for application in anti-inflammatory or wound-dressing treatments.
Institutions: Yeungnam University, King Saud University
Language: English
Subfield: Organic Chemistry
Field: Chemistry
Domain: Physical Sciences
Open Access status: hybrid
Estimated APC paid: $4,390
Awards: G1299250014, G4746520010, G5058288074
OpenAlex ID: W4410216970