Abstract
A series of metronidazole esters have been synthesized starting from metronidazole and various aromatic and aliphatic carboxylic acids using coupling agents such as DCC/DMAP or DIPEA. The synthesized compounds were thoroughly characterized by various spectral data. The melanogenesis activity was determined in mushroom tyrosinase by the oxidation of 3,4-dihydroxyphenylalanine in the presence of the compounds at buffered pH = 6.5 with kojic acid as standard. Among the synthesized compounds, Ia, Ib, and Ih showed moderate activity when compared with the standard IC50 values 94.8, 118.8, and 139,8 ?M, respectively. Molecular docking studies performed with 2y9w protein exhibited a greater number of physical interactions for compounds Ia, Ib, and Ih confirming the mushroom tyrosinase activity.. KEYWORDS :Inhibitors, Melanogenesis, Metronidazole ester, oMlecular docking, Tyrosinase activity.
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