190711-56-9Relevant articles and documents
Neuroprotective effect of novel celecoxib derivatives against spinal cord injury via attenuation of COX-2, oxidative stress, apoptosis and inflammation
An, Yan,Fan, Mingxing,Li, Jianing,Liu, Yajun
, (2020)
A novel series of celecoxib derivatives were synthesized and evaluated for cyclooxygenase (COX-1/COX-2) inhibitory activities for benefit in spinal cord injury (SCI). The title compounds were synthesized by conventional methods in good yields and subsequently tested for inhibitory activity against COX-1/COX-2. The most potent COX-2 inhibitor among the tested derivatives was further assayed for protective effect against experimental SCI of Sprague-Dawley rats. The designed compounds showed considerable inhibition of COX-2 as compared to COX-1 revealing compound 7m as most potent inhibitor of COX-2 isoenzyme (IC50 = 0.04 μM). The expression of mitochondrial apoptotic genes (Bcl-2 and Bax) together with COX-2 and iNOS was restored near to normal as evidenced by western blot analysis in SCI rats. Taken altogether, compound 7m was identified as most potent inhibitor of COX-2. It also showed protective action against SCI via attenuation of COX-2, oxidative stress and apoptosis and inflammation in Male Sprague-Dawley rats.
Preparation method of celecoxib genotoxic impurity
-
, (2020/05/01)
The invention provides a preparation method of a celecoxib genotoxic impurity. The method comprises the following steps: step 1, cyclizing G1 and G2 to generate G3; step 2, carrying out sulfonylationon the G3 to obtain G4; 3, generating G5 by the G4, name
New celecoxib derivatives as anti-inflammatory agents
Szabó, Gy?rgy,Fischer, János,Kis-Varga, ágnes,Gyires, Klára
, p. 142 - 147 (2008/09/19)
A series of 1,5-diarylpyrazoles with a substituted benzenesulfonamide moiety was synthesized and evaluated for cyclooxygenase (COX-1/COX-2) inhibitory activities. Some compounds, for example, (±)-2-[4-(5-p-tolyl-3- trifluoromethyl-pyrazole-1-yl)-benzenesulfonylaminooxy]-propionic acid 16 and its disodium salt 21, had a higher in vivo anti-inflammatory activity compared to celecoxib, despite having no in vitro COX-1 or COX-2 inhibitory activity. Their gastrointestinal side effect profile is essentially more favorable than that of celecoxib.