Details

Autor(en) / Beteiligte

• Janusz, John M
• Young, Patricia A
• Scherz, Michael W
• Enzweiler, Kevin
• Wu, Laurence I
• Gan, Lixian
• Pikul, Stanislaw
• McDow-Dunham, Kelly L
• Johnson, Carl R
• Senanayake, C. B
• Kellstein, David E
• Green, Shelley A
• Tulich, Julie L
• Rosario-Jansen, Theresa
• Magrisso, I. Jack
• Wehmeyer, Kenneth R
• Kuhlenbeck, Deborah L
• Eichhold, Thomas H
• Dobson, Roy L. M

Titel

New Cyclooxygenase-2/5-Lipoxygenase Inhibitors. 2. 7-tert-Butyl-2,3-dihydro-3,3-dimethylbenzofuran Derivatives as Gastrointestinal Safe Antiinflammatory and Analgesic Agents:  Variations of the Dihydrobenzofuran Ring

Ist Teil von

• Journal of medicinal chemistry, 1998-03, Vol.41 (7), p.1124-1137

Ort / Verlag

Washington, DC: American Chemical Society

Erscheinungsjahr

1998

Quelle

MEDLINE

Beschreibungen/Notizen

• A series of 5-keto-substituted 7-tert-butyl-2,3-dihydro-3,3-dimethylbenzofurans (DHDMBFs) were found to be nonsteroidal antiinflammatory and analgesic agents. These compounds are inhibitors of 5-lipoxygenase (5-LOX) and cyclooxygenase (COX) with selectivity for the COX-2 isoform. A series of analogues were prepared to investigate the scope of this lead. Five ketone side chains from active DHDMBFs were used to investigate the effects of changes in the DHDMBF “core”:  the size and identity of the heterocycle and the substituent requirements of the heterocycle and phenyl ring. Biological testing showed that a variety of structural changes can be accommodated, but no structure was clearly superior to the DHDMBF structure.