Synthesis and biological evaluation of polyhydroxy benzophenone as mushroom tyrosinase inhibitors

J Enzyme Inhib Med Chem. 2011 Jun;26(3):449-52. doi: 10.3109/14756366.2010.521745. Epub 2010 Oct 13.


A series of polyhydroxy benzophenone were synthesized and evaluated as mushroom tyrosinase inhibitors. The results demonstrated that most of the target compounds had remarkable inhibitory activities on mushroom tyrosinase. Among all these compounds, 2,3,4,3',4',5'-hexahydroxy-diphenylketone 10 was found to be the most potent tyrosinase inhibitor with IC(50) value of 1.4 μM. In addition, the inhibition kinetics analyzed by Lineweaver-Burk plots revealed that such compounds were competitive inhibitors. These results suggested that such compounds might be utilized for the development of new candidate for treatment of dermatological disorders.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Agaricales / enzymology*
  • Benzophenones / chemistry*
  • Benzophenones / pharmacology*
  • Enzyme Inhibitors / chemical synthesis*
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / pharmacology*
  • Molecular Structure
  • Monophenol Monooxygenase / antagonists & inhibitors*
  • Stereoisomerism
  • Structure-Activity Relationship


  • Benzophenones
  • Enzyme Inhibitors
  • benzophenone
  • Monophenol Monooxygenase