الفهرس 
AcknowledgmentOnly 14 pages are availabe for public view
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Abstract
The introduction of new selective COX-2 inhibitors with high efficacy and enhanced safety profile would be a great achievement in the development of anti-inflammatory drugs. The current 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 in Faculty of Pharmacy, Alexandria University, compared to indomethacin and celecoxib. Twelve compounds were screened for their anti-inflammatory activity using carrageenan-induced paw edema and cotton pellet granuloma tests. Based on their apparent anti-inflammatory activity, 4 drugs with different substitutions were selected for evaluation of their analgesic activity using the formalin-induced hyperalgesia and hot-plate tests. Compound B2 ((4-(3-(4-Methylphenyl)-4-cyano-1H-pyrazol-1-yl)benzenesulfonamide)) showed very promising results. In the single-dose and sub-chronic toxicity studies, compound B2 showed no ulcerogenic effect and produced minimal effects on renal function. Furthermore, compound B2 was less potent inhibitor of COX-2 in-vitro than celecoxib, which may indicate lower potential cardiovascular toxicity. It is concluded that compound B2 could be a promising and safe option for the management of chronic inflammatory conditions. This study recommends more investigation of the therapeutic effects and toxicity profile of this compound including its cardiovascular toxicity.