A novel class of human 15‐LOX‐1 inhibitors based on 3‐hydroxycoumarin

摘要: Inflammations, sensitivities, and some cancers in mammals are intimately linked to the activity of lipo-oxygenase enzymes. Owing importance these enzymes, mechanistic studies, product analysis, synthesis inhibitors have expanded. In this study, a series hydroxycoumarins, methoxy-3-hydroxy coumarins, 7-alkoxy-3-hydroxy coumarins were synthesized evaluated as potential human 15-LOX-1. Among synthetic 7-methoxy-3-hydroxycoumarin derivative demonstrated potent inhibitory compound, 5f, showed best result. Radical scavenging assessment, IC50 , HNMR, DPPH bleaching results indicate that electronic properties major factors for inhibition potency coumarins. Based on theoretical it was suggested mesomeric effect substituent at seventh position benzene ring is one stability oxy-radical intermediate.