The introduction of new COX‐2 inhibitors with high efficacy and enhanced safety profile would be a great achievement in the development of anti‐inflammatory drugs. This study was designed to screen and assess the anti‐inflammatory and analgesic activities as well as some of the expected side effects of some pyrazole derivatives, newly synthesized as potential COX‐2 inhibitors at the Faculty of Pharmacy, Alexandria University and compared to indomethacin and celecoxib. Twelve compounds were screened for their anti‐inflammatory activity using carrageenan‐induced paw oedema and cotton pellet granuloma tests. On the basis of their apparent anti‐inflammatory activity, four compounds with different substitutions were selected for the evaluation of their analgesic activity using the formalin‐induced hyperalgesia and hot‐plate tests. Compound AD 532, ((4‐(3‐(4‐Methylphenyl)‐4‐cyano‐1H‐pyrazol‐1‐yl)benzenesulfonamide)), showed very promising results. In the single‐dose and subchronic toxicity studies, compound AD 532 showed no ulcerogenic effect and produced minimal effects on renal function. Furthermore, compound AD 532 was a less potent inhibitor of COX‐2 in vitro than celecoxib, which may indicate lower potential cardiovascular toxicity. It is concluded that compound AD 532 appears to be a promising and safe option for the management of chronic inflammatory conditions. This study recommends more in‐depth investigation into the therapeutic effects and toxicity profile of this compound including its cardiovascular toxicity.