Abstract
A novel series of 2-pyrazoline derivatives
13a
–
l
was synthesized via aldol condensation of 4-substituted acetophenones with appropriately substituted aldehydes followed by cyclization of the formed chalcones with 4-hydrazinobenzenesulfonamide hydrochloride. The chemical structures of the target pyrazoline derivatives were proved by means of IR,
1
H NMR,
13
C NMR, mass spectroscopy and elemental analyses data. All the synthesized compounds were evaluated for their cyclooxygenase selectivity, anti-inflammatory and ulcerogenic liability. While compounds
13e
,
13h
and
13i
showed moderate COX-2 selectivity in vitro and good anti-inflammatory activity in vivo, compound
13i
showed the highest anti-inflammatory activity that is very close in potency to the reference drug (celecoxib) with better gastric profile than celecoxib.