A scaffold hopping approach to identify novel monoamine oxidase B inhibitors.

A scaffold hopping approach to identify novel monoamine oxidase B inhibitors.

Geldenhuys Werner J; Funk Max O; Van der Schyf Cornelis J; Carroll Richard T

Bioorganic & medicinal chemistry letters

2012

2012-02

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.

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

Article information provided for research and reference use only. All rights are retained by the journal listed under publisher and/or the creator(s).

1380–1383

3

22