Several 1-(1-naphthylacetyl)-3-substituted carbamides were synthesized, characterized, and evaluated for anti-inflammatory and antiproteolytic activity. The protection afforded by most of these carbamides against carrageenan-induced edema in rats at a dose of 100 mg/kg ranged from 4.4 to 50%. Some of these carbamides, which showed higher protection against carrageenan-induced edema, were further evaluated for their antigranulation effect against cotton pellet-induced granuloma formation in rats. All carbamides showed a poor degree of protection against granuloma formation. The antiproteolytic activity of these carbamides, as reflected by their ability to inhibit trypsin-induced hydrolysis of the bovine serum albumin, was of a low order and was unrelated to their anti-inflammatory activity.