European Journal of Medicinal Chemistry p. 159 - 166 (1991)
Update date:2022-08-05
Topics:
Murray, W.V.
Wachter, M.P.
Kasper, A.M.
Argentieri, D.C.
Capetola, R.J.
Ritchie, D.M.
A series of novel 6-(6-alkoxy-2-naphthyl)oxoalkanoates and alkanamides were synthesized as inhibitors of inflammation and 5-lipoxygenase.They were evaluated in vivo for anti-inflammatory activity in the established adjuvent arthritis assay in rats and in vitro as inhibitors of 5-lipoxygenase in rat basophilic leukemia (RBL) cells.N-Hydroxy-N-methyl-6-(6-methoxy-2-naphthyl)-6-oxohexanamide, compound 28, which is representative of the more potent anti-inflammatory / 5-lipogenase inhibitors in the series was approximately twice as potent as the standard, ibuprofen in the adjuvent rat and exhibited an IC50 of 0.25 micromolar in the RBL assay.
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Doi:10.1080/00945719909351735
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