New cyclooxygenase-2/5-lipoxygenase inhibitors. 2. 7-tert-butyl-2, 3-dihydro-3, 3-dimethylbenzofuran derivatives as gastrointestinal safe antiinflammatory and …

…, L Gan, S Pikul, KL McDow-Dunham…

Index: 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. Journal of Medicinal Chemistry, 1998 , vol. 41, # 7 p. 1124 - 1137

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Citation Number: 37

Abstract

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 ...