Synthesis of celecoxib analogues possessing a N-difluoromethyl-1, 2-dihydropyrid-2-one 5-lipoxygenase pharmacophore: biological evaluation as dual inhibitors of cyclooxygenases and 5-lipoxygenase with anti-inflammatory activity
Research Abstract
A novel class of 1-(4-methanesulfonylphenyl and 4-aminosulfonylphenyl)-5-[4-(1-
difluoromethyl-1, 2-dihydropyrid-2-one)]-3-trifluoromethyl-1 H-pyrazole hybrid
cyclooxygenase-2 (COX-2)/5-lipoxygenase (5-LOX) inhibitory anti-inflammatory agents was
designed. Replacement of the tolyl ring present in celecoxib by the N-difluoromethyl-1, 2-
dihydropyrid-2-one moiety provided compounds showing dual selective COX-2/5-LOX
inhibitory activities. 1-(4-Aminosulfonylphenyl)-5-[4-(1-difluoromethyl-1, 2-dihydropyrid-2-
Research Keywords
COX