Trans 2,3-disubstituted-2,3-dihydro-5-hydroxy-benzofurans as inhibitors of leukotriene biosynthesis

摘要

The novel trans-2,3-disubstituted-2,3-­dihydro-5-hydroxybenzofurans are described. The synthesis involves an intramolecular Michael addition to yield the thermodynamic trans isomer. The compounds were found to be inhibitors of 5-lipoxygenase, an enzyme crucial to the biosynthesis of leukotrienes and useful for the treatment of various inflammatory diseases.