Journal
BIOORGANIC CHEMISTRY
Volume 69, Issue -, Pages 29-36Publisher
ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bioorg.2016.09.007
Keywords
1,3,4-Thiadiazole derivatives; Tyrosinase inhibitory activities; Inhibition kinetics; Docking studies
Funding
- Shaoyang University
- Foundation of Education Department of Hunan Province, China [15A172]
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1,3,4-Thiadiazole derivatives bearing Schiff base moieties were designed, synthesized, and their tyrosinase inhibitory activities were evaluated. Some compounds displayed potent tyrosinase inhibitory activities, especially, 4-(((5-mercapto-1,3,4-thiadiazol-2-yl)-imino) methyl)-2-methoxy-phenol (14) exhibited superior inhibitory effect to the other compounds with an IC50 value of 0.036 mu M. The structure-activity relationships (SARs) were preliminarily discussed and docking studies showed compound 14 had strong binding affinity to mushroom tyrosinase. Hydroxy might be the active groups. The inhibition kinetics study revealed that compounds (13 and 14) inhibited tyrosinase by acting as uncompetitive inhibitors. The LD50 value of the compound 14 was 5000 mg/kg. (C) 2016 Elsevier Inc. All rights reserved.
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