Investigation of the anti-inflammatory and analgesic activities of promising pyrazole derivative.

Autor: Bekhit AA; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Alexandria University, Alexandria 21521, Egypt; Pharmacy Program, Pharmacology stream, Allied Health Department, College of Health and Sport Sciences, University of Bahrain, Kingdom of Bahrain. Electronic address: adnbekhit@pharmacy.alexu.edu.eg., Nasralla SN; Pharmacy Program, Pharmacology stream, Allied Health Department, College of Health and Sport Sciences, University of Bahrain, Kingdom of Bahrain., El-Agroudy EJ; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Alexandria University, Alexandria 21521, Egypt., Hamouda N; Department of Clinical Pharmacology, Faculty of Medicine, Alexandria University, Alexandria, Egypt., El-Fattah AA; Department of Materials Science, Institute of Graduate Studies and Research, Alexandria University, Alexandria, 21526, Egypt; Department of Chemistry, College of Science, University of Bahrain, Sakhir P.O. Box. 32038, Kingdom of Bahrain., Bekhit SA; High Institute of Public Health, Alexandria University, Alexandria 21568, Egypt., Amagase K; Laboratory of Pharmacology & Pharmacotherapeutics, College of Pharmaceutical Sciences, Ritsumeikan University, Kusatsu, Shiga, Japan., Ibrahim TM; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Kafrelsheikh University, Kafrelsheikh 33516, Egypt.
Jazyk: angličtina
Zdroj: European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences [Eur J Pharm Sci] 2022 Jan 01; Vol. 168, pp. 106080. Date of Electronic Publication: 2021 Nov 21.
DOI: 10.1016/j.ejps.2021.106080
Abstrakt: The development of new COX-2 inhibitors with analgesic and anti-inflammatory efficacy as well as minimal gastrointestinal, renal and cardiovascular toxicity, is of vital importance to patients suffering from chronic course pain and inflammatory conditions. This study aims at evaluating the therapeutic activity and adverse drug reactions associated with the use of the newly synthesized pyrazole derivative, compound AD732, E-4-[3-(4-methylphenyl)-5-hydroxyliminomethyl-1H-pyrazol-1-yl]benzenesulfonamide, as compared to indomethacin and celecoxib as standard agents. Anti-inflammatory activity was assessed using carrageenan-induced rat paw edema and cotton pellet granuloma tests; formalin-induced hyperalgesia and hot plate tests were done to study analgesic activity. In vitro tests to determine COX-1/COX-2 selectivity and assessment of renal and gastric toxicity upon acute exposure to AD732 were also conducted. Compound AD732 exhibited promising results; higher anti-inflammatory and analgesic effects compared to standard agents, coupled with the absence of ulcerogenic effects and minimal detrimental effects on renal function. Additionally, compound AD732 was a less potent inhibitor of COX-2 in vitro than celecoxib, which may indicate lower potential cardiovascular toxicity. It may be concluded that compound AD732 appears to be a safer and more effective molecule with promising potential for the management of pain and inflammation.
(Copyright © 2021. Published by Elsevier B.V.)
Databáze: MEDLINE
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