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Meri?K?sal, Nesrin G?han, Esra K?eli, Erdem Yesilada, and Hakki Erdogan
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In this study, the synthesis of a novel series Mannich bases of 5-nitro-3-substituted piperazinomethyl-
2-benzoxazolinones are described. The structures attributed to compounds 3a-3k were
elucidated using IR, 1H-NMR spectroscopic techniques besides elemental analysis. The compounds
were examined for their in vivo antiinflammatory and analgesic activities in two different
bioassays, namely, carrageenan-induced hind paw edema and p-benzoquinone-induced
abdominal constriction tests in mice, respectively. In addition, the ulcerogenic effects of the
compounds were determined. Among the tested derivatives most promising results were
obtained for the compounds bearing electron-withdrawing substituents (F, Cl, COCH3) in the
ortho/para position of the phenyl nucleus on the piperazine ring at 3 position of benzoxazolinone
moiety (3a, 3b, 3c, 3d, 3h). The analgesic activities of all compounds are higher than
their antiinflammatory activities. Antiinflammatory inhibitory ratios for all compounds were
above 30% for the last two measurements. Because of this compounds 3a, 3b, 3c, 3d deserve
attention and may be considered for further evaluation.
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