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

Title

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

Creator

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

Publisher

Bioorganic & medicinal chemistry letters

Date

2012
2012-02

Description

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.

Subject

*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

Rights

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

Pages

1380–1383

Issue

3

Volume

22

Citation

Geldenhuys Werner J; Funk Max O; Van der Schyf Cornelis J; Carroll Richard T, “A scaffold hopping approach to identify novel monoamine oxidase B inhibitors.,” NEOMED Bibliography Database, accessed December 7, 2021, https://neomed.omeka.net/items/show/3496.

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