title: Azachalcones: a new class of potent polyphenol oxidase inhibitors.
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 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.
authors.affiliation: School of Chemistry and Forensic Science, University of Technology Sydney, 15 Broadway, Ultimo, NSW 2007, Australia. Electronic address: Sini.KaranayilRadhakrishnan@student.uts.edu.au.
authors.forename: Sini Karanayil
authors.initials: SK
authors.lastname: Radhakrishnan
authors.affiliation: School of Chemistry and Forensic Science, University of Technology Sydney, 15 Broadway, Ultimo, NSW 2007, Australia.
authors.forename: Ronald Gibrial
authors.initials: RG
authors.lastname: Shimmon
authors.affiliation: School of Chemistry and Forensic Science, University of Technology Sydney, 15 Broadway, Ultimo, NSW 2007, Australia.
authors.forename: Costa
authors.initials: C
authors.lastname: Conn
authors.affiliation: School of Chemistry and Forensic Science, University of Technology Sydney, 15 Broadway, Ultimo, NSW 2007, Australia.
authors.forename: Anthony T
authors.initials: AT
authors.lastname: Baker
mesh_terms: D000363:Agaricales / Q000201:enzymology; D001372:Aza Compounds / Q000737:chemistry*; D004156:Catechol Oxidase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D047188:Chalcones / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism; D007700:Kinetics; D007980:Levodopa / Q000737:chemistry / Q000378:metabolism; D014442:Monophenol Monooxygenase / Q000037:antagonists & inhibitors / Q000378:metabolism; D011485:Protein Binding; D013329:Structure-Activity Relationship
chemical_list: D001372:Aza Compounds; D047188:Chalcones; D004791:Enzyme Inhibitors; D007980:Levodopa; D004156:Catechol Oxidase; D014442:Monophenol Monooxygenase
keywords: Azachalcone; Competitive inhibitor; PPO; Tyrosinase