Potent and selective 5-LO inhibitor bearing benzothiophene pharmacophore: Discovery of MK-5286
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- [(1S)-1-hydroxy-1-(trifluoromethyl)propyl]-1H-1,2,3-triazol-1-yl}methyl) -1-benzothiophene-2-carboxamid
NOVEL SUBSTITUTED 1,2,3-TΠAZOLYLMETHYL-BENZOTHIOPHENE OR -INDOLE AND THEIR USE AS LEUKOTΠENE BIOSYNTHESIS INHIBITORS
The instant invention provides compounds of Formula I which are leukotπene biosynthesis inhibitors. Z is a fused (optionally sulfo-oxidized) thiophen ring or a fused pyrrol ring R2-R4 are selected from a variety of substituents Compounds of Formula I are
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(2010/11/25)
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