Anti-inflammatory and antiproteolytic properties of substituted guanidines.

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 carrageenin-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 to 52.0% while such a protection with sodium salicylate (1 mM), used as a reference drug, was 52%. In the present study, the antiproteolytic activity possessed by these compounds was found to bear no relationship with their anti-inflammatory property.

• Authors: V Kishore, S S Parmar, S Kumar, J P Barthwal
• Journal: Pharmacology (Pharmacology) Vol. 15 Issue 2 Pg. 97-103 ( 1977) ISSN: 0031-7012 [Print] Switzerland
• PMID: 847014 (Publication Type: Journal Article)

Chemical References

• Anti-Inflammatory Agents
• Guanidines
• Protease Inhibitors
• Thiourea

Topics

• Animals
• Anti-Inflammatory Agents
• Chemical Phenomena
• Chemistry
• Drug Evaluation, Preclinical
• Edema (drug therapy)
• Guanidines (chemical synthesis, pharmacology, therapeutic use)
• Lethal Dose 50
• Protease Inhibitors
• Rats
• Thiourea