Journal of Medicinal Chemistry p. 3515 - 3529 (1998)
Update date:2022-08-10
Topics:
Janusz, John M.
Young, Patricia A.
Ridgeway, James M.
Scherz, Michael W.
Enzweiler, Kevin
Wu, Laurence I.
Gan, Lixian
Chen, Julian
Kellstein, David E.
Green, Shelley A.
Tulich, Jennifer L.
Rosario-Jansen, Theresa
Magrisso, I. Jack
Wehmeyer, Kenneth R.
Kuhlenbeck, Deborah L.
Eichhold, Thomas H.
Dobson, Roy L. M.
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.
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