New Cyclooxygenase-2/5-Lipoxygenase Inhibitors. 3. 7-tert-Butyl-2,3-dihydro-3,3-dimethylbenzofuran Derivatives as Gastrointestinal Safe Antiinflammatory and Analgesic Agents: Variations at the 5 Position
Journal of Medicinal Chemistry1998Vol. 41(18), pp. 3515–3529
Citations Over Time
John M. Janusz, Patricia A. Young, James M. Ridgeway, Michael W. Scherz, Kevin Enzweiler, Laurence I. Wu, Lixian Gan, Julian Chen, David E. Kellstein, Shelley A. Green, Jennifer L. Tulich, Theresa Rosario-Jansen, I. Jack Magrisso, Kenneth R. Wehmeyer, Deborah L. Kuhlenbeck, Thomas H. Eichhold, Roy L. M. Dobson
Abstract
We report an expansion of the scope of our initial discovery that 5-keto-substituted 7-tert-butyl-2,3-dihydro-3,3-dimethylbenzofurans (DHDMBFs) are antiinflammatory and analgesic agents. Several other functional groups have been introduced at the 5 position: amides, amidines, ureas, guanidines, amines, heterocycles, heteroaromatics, and heteroaryl ethenyl substituents in the 5 position all provide active compounds. These compounds are dual cyclooxygenase (COX) and 5-lipoxygenase (5-LOX) inhibitors. They inhibit both COX-1 and COX-2 with up to 33-fold selectivity for COX-2.
Related Papers
- → Effects of daphnodorin A, B and C, new flavans isolated from traditional Chinese medicine, on the 12-lipoxygenase and cyclooxygenase metabolism of arachidonic acid in rabbit platelets(1998)20 cited
- → Molecular evolution of cyclooxygenase and lipoxygenase(1992)25 cited
- → How specific is the arachidonic acid-induced mouse ear oedema for lipoxygenase (LO)- and cyclooxygenase (CO)-inhibitors?(1986)7 cited
- → Nitric oxide, an inhibition of lipid oxidation by lipoxygenase and cyclooxygenase(1990)
- [The effects of cyclooxygenase and lipoxygenase inhibitors: the prerequisites for more effective anti-inflammatory combinations].(1990)