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Chem Pharm Bull (Tokyo) ; 65(9): 833-839, 2017.
Artículo en Inglés | MEDLINE | ID: mdl-28867710

RESUMEN

The enzyme tyrosinase regulates melanogenesis and skin hyperpigmentation by converting L-3,4-dihydroxyphenylalanine (L-DOPA) into dopaquinone, a key step in the melanin biosynthesis. The present work deals with design and synthesis of various oxindole-based chalcones as monophenolase and diphenolase activity inhibitors of tyrosinase. Among the screened compounds, 4-hydroxy-3-methoxybenzylidene moiety bearing chalcone (7) prepared by one pot reaction of oxindole and vanillin displayed the highest activity against tyrosinase with IC50s of 63.37 and 59.71 µM in monophenolase and diphenolase activity assays, respectively. In molecular docking studies, chalcone 7 also showed the highest binding affinity towards the enzyme tyrosinase while exhibiting the lowest estimated free energy of binding, among all the ligands docked.


Asunto(s)
Chalconas/química , Diseño de Fármacos , Inhibidores Enzimáticos/síntesis química , Monofenol Monooxigenasa/antagonistas & inhibidores , Animales , Benzaldehídos/química , Sitios de Unión , Dominio Catalítico , Chalconas/síntesis química , Chalconas/metabolismo , Inhibidores Enzimáticos/química , Inhibidores Enzimáticos/metabolismo , Indoles/química , Concentración 50 Inhibidora , Melaninas/metabolismo , Simulación del Acoplamiento Molecular , Monofenol Monooxigenasa/metabolismo , Oxindoles , Ratas
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