Synthesis of 4-hydroxy-3-[(E)-2-(6-substituted-9H-purin-9-yl)vinyl]coumarins as lipoxygenase inhibitors

The synthesis of 4-hydroxy-3-[(E)-2-(6-substituted-9H-purin-9-yl)vinyl] coumarins has been achieved from the reactions of 4-hydroxycoumarin with 2-(6-substituted-9H-purin-9-yl)acetaldehydes in DMF under heating. The new compounds showed significant lipoxygenase inhibitory activity (e.g., 6a: IC50 = 6.25 μM).

The synthesized compounds act as lipoxygenase inhibitors.