Safwat M. Rabea, N. El-Koussi, H. Y. Hassan
Jan 1, 2006
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Influential Citations
42
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Quality indicators
Journal
Archiv der Pharmazie
Abstract
A series of 5‐phenyl‐1‐(3‐pyridyl)‐1H‐1,2,4‐triazole‐3‐carboxylic acid derivatives 4–10 were synthesized by rearrangement of 4‐(3‐pyridyl)‐hydrazono‐2‐phenyl‐2‐oxazolin‐5‐one 3 in the presence of different nucleophiles to afford derivatives 4, 7, and 8, while hydroxamic acid derivative 6 was prepared from reaction of methyl ester 4 with hydroxylamine hydrochloride. Semicarbazide 9 and thiosemicarbazide 10, derivatives of the 5‐phenyl‐1‐(3‐pyridyl)‐1H‐1,2,4‐triazole‐3‐carboxylic acid, were synthesized via hydrazide 8 with potassium cyanate and appropriate isothiocyanate, respectively. The structures of the synthesized compounds were confirmed by elemental analyses, IR, 1H‐NMR, and mass spectra. The results of the anti‐inflammatory activity of the synthesized derivatives showed that most of the tested compounds 4–10 showed significant inhibition against carrageenan‐induced rat paw edema in albino rats. Derivatives 4 and 8 showed promising results and were found to be equipotent or more potent than Indomethacin and Celecoxib as reference drugs at two dose levels, 5 and 10 mg/kg, and they have no ulcerogenic activity.