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Inhibition of tyrosinase by 4H‐chromene analogs: Synthesis,kinetic studies,and computational analysis 下载免费PDF全文
Edikarlos M. Brasil Luciana M. Canavieira Érica T. C. Cardoso Edilene O. Silva Jerônimo Lameira José L. M. Nascimento Vera L. Eifler‐Lima Barbarella M. Macchi Dharmarajan Sriram Paul V. Bernhardt José Rogério Araújo Silva Craig M. Williams Cláudio N. Alves 《Chemical biology & drug design》2017,90(5):804-810
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 synthetic heterocyclic compounds behave as competitive inhibitors for the L‐DOPA binding site of the enzyme. Furthermore, molecular modeling provided important insight into the mechanism of binding interactions with the tyrosinase copper active site. 相似文献
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