Molecular docking studies and biological evaluation of 1,3,4-thiadiazole derivatives bearing Schiff base moieties as tyrosinase inhibitors

Compound 14 exhibited most potent tyrosinase inhibitory activity with IC50 value of 0.036μM. The inhibition kinetics study revealed that compounds (13, 14) exhibited such inhibitory effects on tyrosinase by acting as the uncompetitive inhibitors. Docking study was carried out. The LD50 value of the...

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Veröffentlicht in:	Bioorganic chemistry 2016-12, Vol.69, p.29-36
Hauptverfasser:	Tang, Junyuan, Liu, Jinbing, Wu, Fengyan
Format:	Artikel
Sprache:	eng
Schlagworte:	1,3,4-Thiadiazole derivatives Docking studies Dose-Response Relationship, Drug Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology Humans Inhibition kinetics Molecular Docking Simulation Molecular Structure Monophenol Monooxygenase - antagonists & inhibitors Monophenol Monooxygenase - metabolism Schiff Bases - chemical synthesis Schiff Bases - chemistry Schiff Bases - pharmacology Structure-Activity Relationship Thiadiazoles - chemical synthesis Thiadiazoles - chemistry Thiadiazoles - pharmacology Tyrosinase inhibitory activities
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