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Abstract Novel pyrazole and pyrazolo[3,4-d]pyrimidine derivatives were prepared and evaluated for their analgesic activity. The most potent compounds V,Vb, IX, XIId, XIIIc,d, XIVa, XV were further evaluated for their antiinflammatoryactivity. Compounds VIb, IX, XIIIc,d were further evaluated for their ulcerogenic activity. Compounds VIb, IX, XIIId undergo in-vitro COX-II inhibitory activity assay. All Final prepared compounds were studied by molecular docking studies. Compound VIb showed both high analgesic, antiinflammatory, no ulcerogenic effect in addition to its higher selectivity index for COX-II enzyme with SI = 5.1 when comparing to celecoxib with SI = 6.2 exhibiting moderate binding energy -24.12 score Kcal/mol |