Synthesis of Bi-Heterocyclic Sulfonamides as Tyrosinase Inhibitors: Lineweaver–Burk Plot Evaluation and Computational Ascriptions
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چکیده
منابع مشابه
Kojic acid-derived tyrosinase inhibitors: synthesis and bioactivity
Tyrosinase is a key enzyme for melanin biosynthesis, catalyzing the oxidation of L-tyrosine to L-dopaquinone. The tyrosinase inhibition is an effective approach to control hyperpigmentation in human skin and enzymatic browning in fruits and vegetables. Kojic acid is a naturally-occurring tyrosinase inhibitor which has been clinically used to treat the hyperpigmentation of skin. However, kojic a...
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Synthesis and biological evaluation of unsymmetrical curcumin analogues (UCAs) have been achieved. Tyrosinase inhibitory activities were found for most of the prepared synthetic UCAs. Among them, compounds containing 4-hydroxyl-substituted phenolic rings with C-2/C-4- or C-3/C-4-dihydroxyl-substituted diphenolic rings were more active (IC(50) = 1.74~16.74 μM) than 4-butylresorcinol and kojic ac...
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R&D Center, AmorePacific Corporation, Yongin 446-729, Korea. *E-mail: [email protected] †Samkyung Costech Co., Ltd., Suwon 443-734, Korea ‡Department of Bio-Health Technology, College of Biomedical Science, Kangwon National University, Chuncheon 200-701, Korea §Department of Genetic Engineering and Skin Biotechnology Center, College of Life Science, Kyung Hee University, Yongin 446-701, K...
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In the present paper, we report the synthesis and pharmacological evaluation of a new series of azo compounds with different groups (1-naphthol, 2-naphthol, and N,N-dimethylaniline) and trifluoromethoxy and fluoro substituents in the scaffold. All synthesized compounds (5a-5f) showed the most potent mushroom tyrosinase inhibition (IC₅₀ values in the range of 4.39 ± 0.76-1.71 ± 0.49 µM), compara...
متن کاملDesign, synthesis and biological evaluation of hydroxy- or methoxy-substituted phenylmethylenethiosemicarbazones as tyrosinase inhibitors.
A series of hydroxy- or methoxy-substituted phenylmethylenethiosemicarbazones were designed, synthesized and evaluated as mushroom tyrosinase inhibitors. The results demonstrated that most of target compounds had remarkable inhibitory activities on mushroom tyrosinase. Interestingly, compound 2h was found to be the most potent tyrosinase inhibitor with IC50 value of 0.18 microM. The possible in...
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ژورنال
عنوان ژورنال: Acta Chimica Slovenica
سال: 2020
ISSN: 1580-3155
DOI: 10.17344/acsi.2019.5283