Azachalcones: A new class of potent polyphenol oxidase inhibitors. Issue 8 (15th April 2015)

• Record Type: Journal Article
• Authors: Radhakrishnan, Sini Karanayil; Shimmon, Ronald Gibrial; Conn, Costa; Baker, Anthony T.
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 25:Issue 8(2015)
• Page Start: 1753
• Page End: 1756
• Publication Date: 2015-04-15
• Subjects: PPO -- Tyrosinase -- Azachalcone -- Competitive inhibitor; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2015.02.060
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: X = N, Y = CH; IC50 : 1.75 μM. X = CH, Y = N; IC50 : 2.25 μM. Abstract: 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 usingl -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.