200420-91-3Relevant academic research and scientific papers
Dihydrobenzopyran and related compounds useful as anti-inflammatory agents
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, (2008/06/13)
PCT No. PCT/US97/09945 Sec. 371 Date Dec. 7, 1998 Sec. 102(e) Date Dec. 7, 1998 PCT Filed Jun. 6, 1997 PCT Pub. No. WO97/46548 PCT Pub. Date Dec. 11, 1997A compound having structure (1) wherein (a) X is selected from the group consisting of O, S, SO, or S
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
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,Kellstein, David E.,Green, Shelley A.,Tulich, Julie L.,Rosario-Jansen, Theresa,Jack Magrisso,Wehmeyer, Kenneth R.,Kuhlenbeck, Deborah L.,Eichhold, Thomas H.,Dobson, Roy L. M.
, p. 1124 - 1137 (2007/10/03)
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 5-1ipoxygenase (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.
