Protection of carrageenin edema and trypsin hydrolysis of bovine serum albumin by naphthylthiosemicarbazides and their cyclized oxadiazoles.
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.
D000818:Animals; D000893:Anti-Inflammatory Agents; D002351:Carrageenan; D004353:Drug Evaluation, Preclinical; D004487:Edema / Q000139:chemically induced / Q000188:drug therapy*; D006854:Hydrocortisone / Q000627:therapeutic use; D006868:Hydrolysis; D010069:Oxadiazoles / Q000378:metabolism / Q000627:therapeutic use*; D010113:Oxyphenbutazone / Q000627:therapeutic use; D051381:Rats; D012710:Serum Albumin, Bovine / Q000378:metabolism*; D012980:Sodium Salicylate / Q000378:metabolism; D013882:Thiosemicarbazones / Q000378:metabolism / Q000627:therapeutic use*; D014357:Trypsin / Q000494:pharmacology
D000893:Anti-Inflammatory Agents; D010069:Oxadiazoles; D013882:Thiosemicarbazones; D012710:Serum Albumin, Bovine; D002351:Carrageenan; D014357:Trypsin; D010113:Oxyphenbutazone; D006854:Hydrocortisone; D012980:Sodium Salicylate