Abstract
A series of 2,4-diaryl-5(4
H
)-imidazolones were prepared and evaluated for their anti-inflammatory activities. Some selected 2,4-diaryl-5(4
H
)-imidazolones exhibited excellent anti-inflammatory activity in the carrageenan-induced rat paw edema model. Structure Activity Relationships within the series were studied. The substitution at the
N
-sulfonamide moiety by a small hydrophilic acetyl group resulted in compounds with superior
in vivo
anti-inflammatory properties. As expected from their COX-2 selectivity, most of the active compounds lacked gastrointestinal toxicity
in vivo
in rats after a 3-day treatment of 25 mg/kg/day.