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New halogenated phenylcoumarins as tyrosinase inhibitors
Bioorganic & Medicinal Chemistry Letters, 2011With the aim to find out structural features for the tyrosinase inhibitory activity, in the present communication we report the synthesis and pharmacological evaluation of a new series of phenylcoumarin derivatives with different number of hydroxyl or ether groups and bromo substituent in the scaffold.
Matos MJ +7 more
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Synthesis of glabridin derivatives as tyrosinase inhibitors
Archives of Pharmacal Research, 2009A novel 3'',4''-dihydroglabridin was successfully prepared for studying on tyrosinase inhibitory activity. The result demonstrated that 3'',4''-dihydroglabridin exhibited higher activity than glabridin (IC(50) value = 11.40 microM), which is probably due to the 4-substituted resorcinol skeleton and the lacking of double bond between carbon atom 3'' and
Warunee, Jirawattanapong +2 more
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Computational studies of tyrosinase inhibitors
Computational studies have significantly advanced the understanding of tyrosinase (TYR) function, mechanism, and inhibition, accelerating the development of more effective and selective inhibitors. This chapter provides an overview of in silico studies on TYR inhibitors, emphasizing key inhibitory chemotypes and the main residues involved in ligand ...Alessandro, Bonardi, Paola, Gratteri
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Discovery of small-molecule inhibitors of tyrosinase
Bioorganic & Medicinal Chemistry Letters, 2007To identify novel inhibitors of tyrosinase, a fluorescent assay was developed which is suitable for high-throughput screening. In the assay, oxidation of the substrate by tyrosinase leads to the release of a fluorescent coumarin. Several small molecules were identified that inhibited mushroom tyrosinase in vitro and human tyrosinase in cell culture ...
Juris P, Germanas +4 more
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Natural products as tyrosinase inhibitors
Tyrosinase is a crucial copper-containing enzyme involved in the production of melanin. Melasma, age spots, and freckles are examples of hyperpigmentation diseases caused by excess production of melanin. Inhibiting tyrosinase activity is a crucial method for treating these disorders along with various applications such as cosmetics, food technology ...Aslınur, Doğan, Suleyman, Akocak
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Tetraketones: A new class of tyrosinase inhibitors
Bioorganic & Medicinal Chemistry, 2006Twenty-eight tetraketones (1-28) with variable substituents at C-7 were synthesized and evaluated as tyrosinase inhibitors. Remarkably compounds 25 (IC(50)=2.06 microM), 11 (IC(50)=2.09 microM), 15 (IC(50)=2.61 microM), and 27 (IC(50)=3.19 microM) were found to be the most active compounds of the series, even better than both standards kojic acid (IC ...
Khalid Mohammed, Khan +6 more
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Drug design of tyrosinase inhibitors
This copper-containing enzyme catalyzes the rate-limiting step for the melanin skin pigment bioproduction. Tyrosinase inhibitors can be exploited as skin whitening agents and food preservatives, opening new scenarios in food, cosmetics, agriculture and medicine.Melfi F. +4 more
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British Journal of Dermatology, 1981
Purification of tyrosinase inhibitors of hamster melanomas was carried out using tyrosinase binding affinity column chromatography. This method enables the isolation of tyrosinase inhibitors with a 124-fold purification index as compared to that of crude preparation after dialysation.
G, Imokawa, Y, Mishima
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Purification of tyrosinase inhibitors of hamster melanomas was carried out using tyrosinase binding affinity column chromatography. This method enables the isolation of tyrosinase inhibitors with a 124-fold purification index as compared to that of crude preparation after dialysation.
G, Imokawa, Y, Mishima
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