Investigations of new N 1 -substituted pyrazoles as anti-inflammatory and analgesic agents having COX inhibitory activity.
| Autor: | Said MF; Pharmaceutical Chemistry Department, Cairo University, Cairo, 11562, Egypt., George RF; Pharmaceutical Chemistry Department, Cairo University, Cairo, 11562, Egypt., Fayed W; Pharmacognosy Department, Drug Bioassay-Cell Culture, National Research Centre, Dokki, Giza, 12622, Egypt., F Soliman AA; Pharmacognosy Department, Drug Bioassay-Cell Culture, National Research Centre, Dokki, Giza, 12622, Egypt., Refaey RH; Pharmaceutical Chemistry Department, October University for Modern Sciences & Arts. |
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| Jazyk: | angličtina |
| Zdroj: | Future medicinal chemistry [Future Med Chem] 2024 Feb; Vol. 16 (4), pp. 349-368. Date of Electronic Publication: 2024 Jan 30. |
| DOI: | 10.4155/fmc-2023-0302 |
| Abstrakt: | Background: The search is ongoing for ideal anti-inflammatory and analgesic agents with promising potency and reasonable selectivity. Methods: New N 1 -substituted pyrazoles with or without an acetamide linkage were synthesized and evaluated for their anti-inflammatory and analgesic activities. COX inhibitory testing, molecular docking, molecular dynamics simulation and antiproliferative activity assessments were performed. Results: All compounds exhibited anti-inflammatory activity up to 90.40% inhibition. They also exhibited good analgesic activity with up to 100% protection. N 1 -benzensulfonamides 3d , 6c and 6h were preferentially selective agents toward COX-2. Compound 3d showed good cytotoxicity against MCF-7 and HTC116 cancer cell lines. Molecular modeling studies predicted the binding pattern of the most active compounds. Molecular dynamics confirmed the docking results. All compounds showed remarkable pharmacokinetic properties. |
| Databáze: | MEDLINE |
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