Abstract
Sixteen new carboxamide derivatives bearing substituted benzenesulphonamide moiety (7a-p) were synthesized by boric acid mediated amidation of appropriate benzenesulphonamide with 2-amino-4-picoline and tested for anti-inflammatory activity. One compound 7c showed more potent anti-inflammatory activity than celecoxib at 3 h in carrageenan-induced rat paw edema bioassay. Compounds 7g and 7k also showed good anti-inflammatory activity comparable to celecoxib. Compound 7c appeared selectivity index (COX-2/COX-1) better than celecoxib. Compound 7k appeared selectivity index (COX-2/COX-1) a little higher than the half of celecoxib while compound 7g is non-selective for COX-2. The LD50 of compounds 7c, 7g and 7k were comparable to celecoxib.
Highlights
The initial stage of transformation of arachidonic acid to prostanoids are catalysed by cyclooxygenases (COXs)
Nonsteroidal anti-inflammatory drugs (NSAIDs) are the competitive inhibitors of cyclooxygenase (COX), the enzyme which mediates the bioconversion of arachidonic acid to inflammatory prostaglandins (PGs)
The inhibition of COX-2 gives rise to the anti-inflammatory activity of NSAIDs whereas the undesired side effects arise from inhibition of COX-1 activity
Summary
The initial stage of transformation of arachidonic acid to prostanoids are catalysed by cyclooxygenases (COXs). Synthesis of new anti-inflammatory agent comparable to celecoxib inhibitory activity [3]. The slurry was further stirred at Synthesis of new anti-inflammatory agent comparable to celecoxib room temperature for about 4 h.
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