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Anti-Inflammatory, Anti-Allergic, Respiratory & GI Agents

Patent Evaluation: Hydroxamic Acid 5-Lipoxygenase Inhibitors

Pages 1363-1364 | Published online: 02 Mar 2011
 

Summary

Novelty: A novel series of vinylogous hydroxamic acids are claimed along with their methods of preparation and their use in the treatment of inflammatory diseases, such as rheumatoid arthritis and psoriasis.

Biology: Data are given for nineteen compounds in a RBL-1 5-lipoxygenase assay with IC50s in the range 0.06–7.7 μM. The most potent compound is said to be 1-(4-biphenyl)-3-(N-hydroxy-N-methyl)aminoprop-2-en-1-one.

Chemistry: Experimental details and physical data are given for twenty-nine examples with the preferred compounds having the aromatic ring substituted with a halogen, nitro or phenyl group. No compounds are specifically claimed.

Structure:

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