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/

We report an expansion of the scope of our initial discovery that 5-ke to-substituted 7-tert-butyl-2,3-dihydro-3,3-dimethylbenzofurans (DHDMB Fs) are antiinflammatory and analgesic agents. Several other functiona l groups have been introduced at the 5 position: amides, amidines, ure as, guanidines, amines, heterocycles, heteroaromatics, and heteroaryl ethenyl substituents in the 5 position all provide active compounds. T hese compounds are dual cyclooxygenase (COX) and 5-lipoxygenase (5-LOX ) inhibitors. They inhibit both COX-1 and COX-2 with up to 33-fold sel ectivity for COX-2.