Selective inhibition of cyclooxygenase 2
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Cited by (145)
Nimesulide analogues: From anti-inflammatory to antitumor agents
2019, Bioorganic ChemistryCitation Excerpt :The A’ position was also modified and it was demonstrated that the oxime, 1-hydroxyethyl and 1-aminoethyl analogues showed moderate to excellent anti-inflammatory activity [79]. Flosulide (Fig. 2) is considered a selective COX-2 inhibitor with an IC50 value of 14.7 nM [110]. Further studies aiming to develop flosulide analogues starting from safrole were performed and the results evidenced that two derivatives with a N-methylsulfonamide moiety (Fig. 3A) and the corresponding retrosulfonamide group (Fig. 3B) were more active than nimesulide, having an inhibition of 46% and 43.1% at a dose of 100 µmol/Kg, respectively, in a carrageenan-induced pleurisy assay [76].
Assessment of common Nonsteroidal anti-inflammatory medications by whole blood aggregometry: A clinical evaluation for the perioperative setting
2014, World NeurosurgeryCitation Excerpt :The COX-2 enzyme is typically found within macrophages after inflammatory induction. It is assumed that there is little to no effect on platelets with the use of the COX-2 medications (14, 18, 21, 33, 35), although some newer medications have been found to retain some platelet TXA2 inhibitory properties, generally on several orders of magnitude lower than the conventional NSAIDs (14, 33). There is little multidisciplinary literature correlating non-ASA NSAID use with perioperative bleeding.
Perioperative Administration of Selective Cyclooxygenase-2 Inhibitors for Postoperative Pain Management in Patients After Total Knee Arthroplasty
2013, Journal of ArthroplastyCitation Excerpt :Previous studies have shown that conventional preoperative use of nonselective NSAIDs increase bleeding risks [43,44]. Conventional nonselective NSAIDs reversibly inhibit COX and interfere with platelet functions, whereas selective COX-2 inhibitors have less antiplatelet effects than conventional nonselective NSAIDs [45,46]. Analysis of 4 studies shows no difference in blood loss between groups [19,22,28,29], thus confirming indirectly that selective COX-2 inhibitors have little effect on serum thromboxane or platelet functions [18].
European perspectives on upcoming analgesics: What do they have that we don't-and what do they think about them?
2010, Techniques in Regional Anesthesia and Pain ManagementCitation Excerpt :Diclofenac has an acidity constant of 4.0, a partition coefficient of 13.4, and structural elements that include a phenyacetic acid group, a secondary amino group, and a phenyl ring containing chlorine atoms, which induce a large angle of torsion between the rings. Alteration of any of these elements in analogs results in a decrease in biological activity.61 Diclofenac produces a relatively nonselective inhibition of the cyclooxygenase isozymes COX-1 and COX-2 (the measured ratio of selectivity for COX-2 over COX-1 ranges from about 1.4-to about 26-fold in the studies cited).
Characterization of Eltenac and novel COX-2 selective thiopheneacetic acid analogues in vitro and in vivo
2008, Biochemical PharmacologyThe role of the cylooxygenase pathway in nociception and pain
2006, Seminars in Cell and Developmental Biology