Journal
BIOORGANIC CHEMISTRY
Volume 86, Issue -, Pages 459-472Publisher
ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bioorg.2019.01.036
Keywords
Thiazole; Triazole; Acetamides; Tyrosinase; Melanogenesis; Hemolytic; Binding energy
Funding
- Basic Science Research Program through the National Research Foundation of Korea (NRF) - Ministry of Education [2017R1D1A1B03034948]
- National Research Foundation of Korea [2017R1D1A1B03034948] Funding Source: Korea Institute of Science & Technology Information (KISTI), National Science & Technology Information Service (NTIS)
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The present research was designed for the selective synthesis of novel bi-heterocyclic acetamides, 9a-n, and their tyrosinase inhibition to overwhelm the problem of melanogenesis. The structures of newly synthesized compounds were confirmed by spectral techniques such as H-1 NMR, C-13 NMR, and EI-MS along with elemental analysis. The inhibitory effects of these bi-heterocyclic acetamides (9a-n) were evaluated against tyrosinase and all these molecules were recognized as potent inhibitors relative to the standard used. The Kinetics mechanism was analyzed by Lineweaver-Burk plots which explored that compound, 9h, inhibited tyrosinase competitively by forming an enzyme-inhibitor complex. The inhibition constants K-i calculated from Dixon plots for this compound was 0.0027 mu M. The computational study was coherent with the experimental records and these ligands exhibited good binding energy values (kcal/mol). The hemolytic analysis revealed their mild cytotoxicity towards red blood cell membranes and hence, these molecules can be pondered as nontoxic medicinal scaffolds for skin pigmentation and related disorders.
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