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  • Title: Antiinflammatory and antiproteolytic properties of naphthlthiosemicarbazides and cyclized oxadiazoles.
    Author: Kishore V, Kumar S, Parmar SS, Senberg VI.
    Journal: Res Commun Chem Pathol Pharmacol; 1975 Aug; 11(4):581-94. PubMed ID: 1179029.
    Abstract:
    Eight 1-(naphth-1-ylacetyl)-4-substituted thiosemicarbazides and eight 2-(naphth-1-ylmethyl)-5-arylamino-1,3,4-oxadiazoles were synthesized and evaluated for antiinflammatory and antiproteolytic properties. All thiosemicarbazides (100 mg/kg) provided 14-43% protection against carrageenin-induced edema in rats. Cyclization of thiosemicarbazides to oxadiazoles resulted in significant reduction in the antiinflammatory activity. Some of these thiosemicarbazides also possessed low antiinflammatory activity against cotton-pellet-induced granuloma formation and formaldehyde-induced arthritis in rats. Hydrocortisone and oxyphenbutazone, used as reference drugs, exhibited greater antiinflammatory activity. All compounds possessed antiproteolytic activity. The in vitro protection of trypsin-induced hydrolysis of bovine serum albumin, unlike antiinflammatory activity, was greater with oxadiazoles (30-90%) than the precursor thiosemicarbazides (4-50%) at a final concentration of 1 mM.
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