Design, Synthesis and Biological Evaluation of Hydroxy- or Methoxy-Substituted Phenylmethylenethiosemicarbazones as Tyrosinase Inhibitors

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  • Yi Wei
    School of Chemistry and Chemical Engineering, Sun Yat-sen University
  • Cao Ri-Hui
    School of Chemistry and Chemical Engineering, Sun Yat-sen University
  • Chen Zhi-Yong
    School of Chemistry and Chemical Engineering, Sun Yat-sen University
  • Yu Liang
    School of Chemistry and Chemical Engineering, Sun Yat-sen University
  • Ma Lin
    School of Chemistry and Chemical Engineering, Sun Yat-sen University
  • Song Hua-Can
    School of Chemistry and Chemical Engineering, Sun Yat-sen University

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Description

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 μM. The possible interaction mode between compound 2h and tyrosinase was proposed. In addition, the 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activities of select compounds (IC50<10.0 μM) were also investigated. Compounds 2d, 2e, 2h, 2i and 2l exhibited more potent DPPH radical scavenging activity than well-known antioxidants ascorbic acid (Vc) and tertiary butyl hydroquinone (TBHQ). These results suggested that such compounds might be utilized for the development of new candidate for treatment of dermatological disorders.

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