Anti-Inflammatory and Antiproteolytic Properties of Substituted Guanidines

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Abstract
Ten N-(4-propoxyphenyl)-N''-(4-chlorophenethyl)-N"-substituted guanidines were synthesized from the corresponding 1-(4-propoxyphenyl)-3-substituted thiocarbamides and evaluated for anti-inflammatory and antiproteolytic properties. All substituted guanidines (50 mg/kg) provided 1-31% protection against carrageenan-induced edema in rats. Hydrocortisone (10 mg/kg) and oxyphenbutazone (40 mg/kg), used as reference drugs, exhibited greater anti-inflammatory activity. All substituted guanidines (1 mM) possessed antiproteolytic activity. The degree of protection observed by these compounds against trypsin-induced hydrolysis of bovine serum albumin ranged from 12.9-52.0% while such a protection with sodium salicylate (1 mM), used as a reference drug, was 52%. The antiproteolytic activity possessed by these compounds bore no relationship with their anti-inflammatory property.

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