title: New halogenated phenylcoumarins as tyrosinase inhibitors.
abstract: With the aim to find out structural features for the tyrosinase inhibitory activity, in the present communication we report the synthesis and pharmacological evaluation of a new series of phenylcoumarin derivatives with different number of hydroxyl or ether groups and bromo substituent in the scaffold. The synthesized compounds 5-12 were evaluated as mushroom tyrosinase inhibitors showing, two of them, lower IC(50) than the umbelliferone. Compound 12 (IC(50)=215 μM) is the best tyrosinase inhibitor of this series.
authors.affiliation: Departamento de Química Orgánica, Facultad de Farmacia, Universidad de Santiago de Compostela, 15782 Santiago de Compostela, Spain. mariacmatos@gmail.com
authors.forename: Maria João
authors.initials: MJ
authors.lastname: Matos
authors.forename: Lourdes
authors.initials: L
authors.lastname: Santana
authors.forename: Eugenio
authors.initials: E
authors.lastname: Uriarte
authors.forename: Giovanna
authors.initials: G
authors.lastname: Delogu
authors.forename: Marcella
authors.initials: M
authors.lastname: Corda
authors.forename: Maria Benedetta
authors.initials: MB
authors.lastname: Fadda
authors.forename: Benedetta
authors.initials: B
authors.lastname: Era
authors.forename: Antonella
authors.initials: A
authors.lastname: Fais
mesh_terms: D000363:Agaricales / Q000201:enzymology; D001966:Bromine / Q000737:chemistry*; D003374:Coumarins / Q000737:chemistry* / Q000494:pharmacology*; D004789:Enzyme Activation / Q000187:drug effects; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D014442:Monophenol Monooxygenase / Q000037:antagonists & inhibitors*
chemical_list: D003374:Coumarins; D004791:Enzyme Inhibitors; C094411:4-phenylcoumarin; D014442:Monophenol Monooxygenase; D001966:Bromine