RESUMEN
In the present study, ten new substituted 3-hydroxypyridine-4-one derivatives were synthesized in a four-step method, and their chemical structures were confirmed using various spectroscopic techniques. Subsequently, the inhibitory activities of these derivatives against tyrosinase enzyme and their antioxidant activities were evaluated. Amongest the synthesized compounds, 6b bearing a 4-OH-3-OCH3 substitution was found to be a promising tyrosinase inhibitor with an IC50 value of 25.82 µM, which is comparable to the activity of kojic acid as control drug. Kinetic study indicated that compound 6b is a competitive inhibitor of tyrosinase enzyme, which was confirmed by molecular docking results. The molecular docking study and MD simulation showed that compound 6b was properly placed within the tyrosinase binding pocket and interacted with key residues, which is consistent with its biological activity. The DFT analysis demonstrated that compound 6b is kinetically more stable than the other compounds. In addition, compounds 6a and 6b exhibited the best antioxidant activities. The findings indicate that compound 6b could be a promising lead for further studies.
RESUMEN
This article describes the synthesis of a novel Yolk-Shell structured Magnetic Yolk-Shell Nanomaterials Modified by Functionalized Carbon Shell with Schiff/Palladium Bases (Fe3O4@void@C-Schiff-base/Pd). The designed Fe3O4@void@C-Schiff-base/Pd catalyst was characterized using several techniques such as Fourier transform infrared spectroscopy (FTIR), vibrating sample magnetometry (VSM), scanning electron microscopy (SEM), energy dispersive X-ray spectroscopy (EDX), thermal gravimetric analysis (TGA), powder X-ray diffraction (PXRD) and Inductively coupled plasma (ICP). The Fe3O4@void@C-Schiff-base/Pd was used as powerful catalyst for preparation Suzuki reaction in short reaction times and high yield in H2O at 60 °C and presence of potassium carbonate base. This nanocatalyst was magnetically recovered and reused several times with keeping its efficiency.