A scaffold hopping approach to identify novel monoamine oxidase B inhibitors

Bioorg Med Chem Lett. 2012 Feb 1;22(3):1380-3. doi: 10.1016/j.bmcl.2011.12.056. Epub 2011 Dec 16.

Abstract

Monoamine oxidase B (MAO-B) inhibitors are used to treat Parkinson's disease. In this study, we searched for novel MAO-B inhibitors using a scaffold hopping approach based on our experience with the thiazolidinedione (TZD) class of compounds as MAO-B inhibitors. Several novel compounds were identified, with potencies in the low nanomolar and low micromolar range. We also found that derivatives of the natural product sulfuretin are potent MAO-A and MAO-B inhibitors.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Benzofurans / chemistry
  • Benzofurans / pharmacology
  • Enzyme Activation / drug effects
  • Flavonoids / chemistry
  • Flavonoids / pharmacology
  • Humans
  • Inhibitory Concentration 50
  • Models, Molecular
  • Molecular Structure
  • Monoamine Oxidase Inhibitors / chemistry*
  • Monoamine Oxidase Inhibitors / pharmacology*
  • Monoamine Oxidase* / chemistry
  • Monoamine Oxidase* / metabolism
  • Protein Binding / drug effects
  • Small Molecule Libraries
  • Structure-Activity Relationship

Substances

  • Benzofurans
  • Flavonoids
  • Monoamine Oxidase Inhibitors
  • Small Molecule Libraries
  • Monoamine Oxidase
  • sulfuretin