Anti-Inflammatory/5-Lipoxygenase Inhibitors, Cyclooxygenase Inhibitors: Dual Cyclooxygenase/5-Lipoxygenase Inhibitors Designed from NSAIDs

Summary

Novelty: N-Hydroxy derivatives of selected non-steroidal anti-inflammatory drugs (fenamate, indomethacin, cycloprofen, oxapinac and indoprofen) which act as dual or selective inhibitors of 5-lipoxygenase and cyclooxygenase are disclosed. They are useful in the treatment of inflammation, arthritis, pain, fever etc.

Biology: Data are presented from various standard test procedures for 5-lipoxygenase and cyclooxygenase inhibition. LTB₄ and PGF_2α radio immunoassays are used and the results expressed as IC₅₀ values (amount of test compound causing 50% inhibition of LTB₄ or PGF_2α formation) or as a percentage inhibition.

Chemistry: N-[[2-[(2,6-Dichloro-3-methylphenyl)amino]phenyl]-methyl]-N-hydroxy acetamide is one of twenty specifically claimed compounds.