Potent and selective 5-LO inhibitor bearing benzothiophene pharmacophore: Discovery of MK-5286 ☆

Abstract The strategy and SAR studies that led to the discovery of a novel potent and orally available 5-lipoxygenase (5-LO) inhibitor 3-(4-fluorophenyl)-6-({4-[(1 S )-1-hydroxy-1-(trifluoromethyl)propyl]-1 H -1,2,3-triazol-1-yl}methyl)-1-benzothiophene-2-carboxamide (( S )- 2l or MK-5286 ) were described.