期刊
CHEMICAL BIOLOGY & DRUG DESIGN
卷 90, 期 5, 页码 804-810出版社
WILEY
DOI: 10.1111/cbdd.13001
关键词
inhibitor; kinetic assays; kojic acid; molecular modeling; multicomponent reaction; tyrosinase
资金
- Conselho Nacional de Desenvolvimento Cientifico e Tecnologico (CNPq)
- Coordenacao de Aperfeicoamento de Pessoal de Nivel Superior (CAPES)
- University of Queensland
- Australian Research Council (ARC) [FT110100851]
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 K-i value of 4m, 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.
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