Inhibition of tyrosinase by 4H‐chromene analogs: Synthesis, kinetic studies, and computational analysis

Inhibition of mushroom tyrosinase was observed with synthetic dihydropyrano[3,2‐b]chromenediones. Among them, DHPC04 displayed the most potent tyrosinase inhibitory activity with a Ki value of 4 μm, comparable to the reference standard inhibitor kojic acid. A kinetic study suggested that these synth...

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Veröffentlicht in:	Chemical biology & drug design 2017-11, Vol.90 (5), p.804-810
Hauptverfasser:	Brasil, Edikarlos M., Canavieira, Luciana M., Cardoso, Érica T. C., Silva, Edilene O., Lameira, Jerônimo, Nascimento, José L. M., Eifler‐Lima, Vera L., Macchi, Barbarella M., Sriram, Dharmarajan, Bernhardt, Paul V., Silva, José Rogério Araújo, Williams, Craig M., Alves, Cláudio N.
Format:	Artikel
Sprache:	eng
Schlagworte:	Agaricales - drug effects Agaricales - enzymology Benzopyrans - chemical synthesis Benzopyrans - chemistry Benzopyrans - pharmacology Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology inhibitor kinetic assays Kinetics kojic acid Models, Molecular molecular modeling Monophenol Monooxygenase - antagonists & inhibitors Monophenol Monooxygenase - metabolism multicomponent reaction Pyrones - pharmacology Structure-Activity Relationship tyrosinase
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