1,2,3‐Triazole‐linked 5‐benzylidene (thio)barbiturates as novel tyrosinase inhibitors and free‐radical scavengers
Sign Up to like & getrecommendations! Published in 2020 at "Archiv der Pharmazie"
DOI: 10.1002/ardp.202000058
Abstract: In this study, benzyl‐1,2,3‐triazole‐linked 5‐benzylidene (thio)barbiturate derivatives 7a–d and 8a–h were designed as potential tyrosinase inhibitors and free‐radical scavengers. The twelve derivatives were synthesized via the [3+2] cycloaddition reaction of the corresponding benzyl azide as… read more here.
Keywords: linked benzylidene; triazole linked; tyrosinase inhibitors; free radical ... See more keywords
Novel 1,2,4-triazole analogues as mushroom tyrosinase inhibitors: synthesis, kinetic mechanism, cytotoxicity and computational studies
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DOI: 10.1007/s11030-020-10102-5
Abstract: We have created a novel series of mushroom tyrosinase inhibitors with 1,2,4-triazole as fundamental skeleton. The target compound 1,2,4-triazol-3-ylthio)- N -phenyl acetamide derivatives 9(a–l) were synthesized by the reaction of 4- and 5-substituted 1,2,4-triazole-3-thiol derivatives… read more here.
Keywords: tyrosinase inhibitors; tyrosinase; mushroom tyrosinase; cytotoxicity ... See more keywords
In vitro biological evaluation and molecular docking studies of natural and semisynthetic flavones from Gardenia oudiepe (Rubiaceae) as tyrosinase inhibitors.
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DOI: 10.1016/j.bioorg.2018.10.034
Abstract: Hyperpigmentation disorders are difficult to treat without causing permanent depigmentation or irritation. The most effective hypopigmenting agents are tyrosinase inhibitors, however some of those currently used have shown serious side effects. As several classes of… read more here.
Keywords: docking studies; gardenia oudiepe; tyrosinase inhibitors; molecular docking ... See more keywords
1,2,3-Triazole-based kojic acid analogs as potent tyrosinase inhibitors: Design, synthesis and biological evaluation.
Sign Up to like & getrecommendations! Published in 2019 at "Bioorganic chemistry"
DOI: 10.1016/j.bioorg.2018.10.069
Abstract: A series of kojic acid-derived compounds 6a-p bearing aryloxymethyl-1H-1,2,3-triazol-1-yl moiety were designed by modifying primary alcoholic group of kojic acid as tyrosinase inhibitors. The target compounds 6a-p were synthesized via click reaction. All compounds showed… read more here.
Keywords: analogs potent; based kojic; tyrosinase inhibitors; kojic acid ... See more keywords
Tyrosinase inhibitors as potential antibacterial agents.
Sign Up to like & getrecommendations! Published in 2019 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2019.111892
Abstract: Tyrosinase is a copper-containing enzyme that catalyzes the biosynthesis of melanin. This enzyme is present in bacteria, fungi, plants and animals, and plays multiple roles in pigmentation, wound healing, radiation protection, primary immune responses and… read more here.
Keywords: potential antibacterial; antibacterial agents; tyrosinase inhibitors; tyrosinase ... See more keywords
Facile synthesis of new quinazolinone benzamides as potent tyrosinase inhibitors: Comparative spectroscopic and molecular docking studies
Sign Up to like & getrecommendations! Published in 2019 at "Journal of Molecular Structure"
DOI: 10.1016/j.molstruc.2019.126915
Abstract: Abstract The simple reaction approach has been designed and utilized for the synthesis of quinazolinone benzamides 4a-4h using isatoic anhydride, m-Anisic hydrazide and various aldehydes. The formation of target compounds was confirmed by spectral characterization… read more here.
Keywords: facile synthesis; tyrosinase inhibitors; quinazolinone benzamides; fluorescence ... See more keywords
Advances in the Design of Genuine Human Tyrosinase Inhibitors for Targeting Melanogenesis and Related Pigmentations.
Sign Up to like & getrecommendations! Published in 2020 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.0c00994
Abstract: Human tyrosinase (hsTYR) is the key enzyme ensuring the conversion of L-tyrosine to dopaqui-none, thereby initiating melanin synthesis, i.e. melanogenesis. Although the protein has long been familiar, knowledge about its three-dimensional structure and efficient overexpression… read more here.
Keywords: tyrosinase inhibitors; chemistry; tyrosinase; advances design ... See more keywords
Design, Synthesis, and Structural Characterization of Thioflavones and Thioflavonols as Potential Tyrosinase Inhibitors: In Vitro and In Silico Studies
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DOI: 10.1021/acsomega.2c01841
Abstract: To find new potential tyrosinase inhibitors, a diverse range of 2-arylchromone-4-thione derivatives (2a–2p) were designed and synthesized by employing a multistep strategy, and the newly synthesized compounds, for the first time, were screened in vitro… read more here.
Keywords: thioflavones thioflavonols; design synthesis; potential tyrosinase; tyrosinase inhibitors ... See more keywords
Evaluation of 2,3-Dihydro-1,5-benzothiazepine Derivatives as Potential Tyrosinase Inhibitors: In Vitro and In Silico Studies
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DOI: 10.1021/acsomega.3c01566
Abstract: Benzothiazepines are pharmacologically active compounds, frequently utilized as a precursor for acquiring versatile molecules with several bioactivities including anti-inflammatory, anti-human immunodeficiency virus (anti-HIV), analgesic, antitumor, antimicrobial, and antitubercular. In this study, the 2,4-diphenyl-2,3-dihydro-1,5-benzothiazepine scaffold was… read more here.
Keywords: silico studies; dihydro benzothiazepine; benzothiazepine; tyrosinase inhibitors ... See more keywords
Synthesis of Bi-heterocyclic Sulfonamides as Tyrosinase Inhibitors: Lineweaver-Burk Plot Evaluation and Computational Ascriptions.
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DOI: 10.17344/acsi.2019.5283
Abstract: The designed bi-heterocyclic sulfonamides were synthesized through a two-step protocol and their structures were ascertained by spectral techniques including IR, 1H NMR and 13C NMR along with CHN analysis. The in vitro inhibitory effects of… read more here.
Keywords: sulfonamides tyrosinase; lineweaver burk; tyrosinase inhibitors; synthesis heterocyclic ... See more keywords
Advances in the tyrosinase inhibitors from plant source.
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DOI: 10.2174/0929867325666180522091311
Abstract: Tyrosinase is a multifunctional copper-containing oxidase which catalyses the oxidation of tyrosine to produce melanin. The alteration in melanin biosynthesis occurs in many diseases. The pigment has a protecting role against skin photo-carcinogenesis, but anomalous… read more here.
Keywords: plant source; advances tyrosinase; tyrosinase inhibitors; inhibitors plant ... See more keywords