Abstract
Novel series of pyrazolo[5,1- b]1,3-oxazolidines, pyrazolo[5,1- b]1,3-oxazines and imidazolidino[1,2- d]pyrazoles were synthesized. These compounds were evaluated in vitro for their ability to inhibit cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) in human whole blood (HWB). Several of the compounds were found to be novel and selective COX-2 inhibitors, the most potent and selective being 1-(5-cyclohexyl (2H,3H-pyrazolo[5,1- b]-1,3-oxazolidin-6-yl)-4-(methylsulfonyl)benzene, 7a (IC 5o for COX-1>100 μM; for COX-2=1.3 μM).
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