Syntheses and Auti-inflammatory Activity of Novel Oximes and O-Acyloximes

概要

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Novel oximes were prepared from the corresponding aldehyde or ketone in the usual way, and a number of oxime esters, O-lauroyl, O-2-pyridinecarbonyl, O-nicotinoyl and O-isonicotinoyl oximes were sgnthesized by 1-ethyl-3-(3-dimethylaminopropyl)carbodiimede (EDCI)-4-dimethylaminopyridine (DMAP) method or a mixed anhydride method, in our search for potent anti-inflammatory compounds. The anti-inflammatory activity of these compounds was assessed by the carrageenan-induced paw edema assay in rats. The oximes (4,5,and 13), O-lauroyloxime 1L, O-nicotinoyloximes (1N, 2N, 3N, and 4N), O-isonicotinoyloxime 1I, and O-2-pyridinecarbonyloxime 7P showed higher anti-inflammatory potency than aspirin, a prostaglandin cyclooxygenase inhibitor.
社団法人日本薬学会の論文
1992-09-25