Azachalcones: A new class of potent polyphenol oxidase inhibitors

A library of potent inhibitors of polyphenol oxidase and their structure activity relationships are described. Azachalcone derivatives were synthesized and tested for their tyrosinase inhibitory activity. Their inhibitory activities on mushroom tyrosinase using l-DOPA as a substrate were investigated. Two compounds that are the reduction congeners of the pyridinyl azachalcones strongly inhibited the enzyme activity and were more potent than the positive control kojic acid.

X = N, Y = CH; IC50: 1.75 μM.X = CH, Y = N; IC50: 2.25 μM.Figure optionsDownload as PowerPoint slide