title: 1-(1-Arylethylidene)thiosemicarbazide derivatives: a new class of tyrosinase inhibitors.
abstract: A series of 1-(1-arylethylidene)thiosemicarbazide compounds and their analogues were synthesized and characterized by 1H NMR, MS. Their tyrosinase inhibitory activities were investigated by an assay based on the catalyzing ability of tyrosinase for the oxidation of L-DOPA, comparing with 4-methoxycinnamic acid and arbutin. The results showed that (1) all the synthesized compounds could perform a significant inhibitory activity for tyrosinase; (2) for these compounds, the main active moiety interacting with the center of tyrosinase would be thiosemicarbazo group; (3) the inhibitory activity was close related with thiosemicarbazide moieties and the groups attached on the aromatic ring.
authors.affiliation: School of Chemistry and Chemical Engineering, Sun Yat-sen University, Guangzhou 510275, China.
authors.forename: Jinbing
authors.initials: J
authors.lastname: Liu
authors.forename: Wei
authors.initials: W
authors.lastname: Yi
authors.forename: Yiqian
authors.initials: Y
authors.lastname: Wan
authors.forename: Lin
authors.initials: L
authors.lastname: Ma
authors.forename: Huacan
authors.initials: H
authors.lastname: Song
mesh_terms: D001665:Binding Sites; D004789:Enzyme Activation / Q000187:drug effects; D015394:Molecular Structure; D010455:Peptides / Q000737:chemistry* / Q000145:classification / Q000494:pharmacology*; D012663:Semicarbazides / Q000737:chemistry* / Q000145:classification / Q000494:pharmacology*
chemical_list: D010455:Peptides; D012663:Semicarbazides; C005151:thiosemicarbazide