Protection of carrageenin edema and trypsin hydrolysis of bovine serum albumin by naphthylthiosemicarbazides and their cyclized oxadiazoles.

Abstract

Seven 1-(naphth-1-ylacetyl)-4-substituted thiosemicarbazides were synthesized and cyclized to the corresponding 2-(naphth-1-ylmethyl)-5-arylamino-1,3,4-oxadiazoles. All compounds, with the exception of two slbstituted oxadiazoles, possessed low anti-inflammatory activity. The protection afforded by these compounds against carrageen-in-induced edema ranged from 3 to 43% where cyclization, in general, decreased anti-inflammatory activity. All compounds (1 mM), possessed antiproteolytic activity where in vitro protection of trypsin-induced hydrolysis of bovine serum albumin, in most cases was greater with oxadiazoles.

• Authors: V Kishore, S Kumar, N K Narain, S S Parmar, V I Stenberg
• Journal: Pharmacology (Pharmacology) Vol. 14 Issue 5 Pg. 390-6 ( 1976) ISSN: 0031-7012 [Print] Switzerland
• PMID: 1031213 (Publication Type: Journal Article, Research Support, U.S. Gov't, Non-P.H.S., Research Support, U.S. Gov't, P.H.S.)

Chemical References

• Anti-Inflammatory Agents
• Oxadiazoles
• Thiosemicarbazones
• Serum Albumin, Bovine
• Carrageenan
• Trypsin
• Oxyphenbutazone
• Hydrocortisone
• Sodium Salicylate

Topics

• Animals
• Anti-Inflammatory Agents
• Carrageenan
• Drug Evaluation, Preclinical
• Edema (chemically induced, drug therapy)
• Hydrocortisone (therapeutic use)
• Hydrolysis
• Oxadiazoles (metabolism, therapeutic use)
• Oxyphenbutazone (therapeutic use)
• Rats
• Serum Albumin, Bovine (metabolism)
• Sodium Salicylate (metabolism)
• Thiosemicarbazones (metabolism, therapeutic use)
• Trypsin (pharmacology)