Protection of Carrageenin Edema and Trypsin Hydrolysis of Bovine Serum Albumin by Naphthylthiosemicarbazides and their Cyclized Oxadiazoles

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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 2 substituted oxadiazoles, possessed low anti-inflammatory activity. The protection afforded by these compounds against [rat] carrageenin-induced edema ranged from 3-43% and cyclization generally decreased the anti-inflammatory activity. All compounds (1 mM) possessed antiproteolytic activity in in vitro protection of trypsin-induced hydrolysis of bovine serum albumin; in most cases this was greater with the oxadiazoles.

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