Structure-activity relationship and docking studies of thiazolidinedione-type compounds with monoamine oxidase B.

Title

Structure-activity relationship and docking studies of thiazolidinedione-type compounds with monoamine oxidase B.

Creator

Carroll Richard T; Dluzen Dean E; Stinnett Hilary; Awale Prabha S; Funk Max O; Geldenhuys Werner J

Publisher

Bioorganic & medicinal chemistry letters

Date

2011
2011-08

Description

The neuroprotective activity of pioglitazone and rosiglitazone in the MPTP parkinsonian mouse prompted us to evaluate a set of thiazolidinedione (TZD) type compounds for monoamine oxidase A and B inhibition activity. These compounds were able to inhibit MAO-B over several log units of magnitude (82 nM to 600 muM). Initial structure-activity relationship studies identified key areas to modify the aromatic substituted TZD compounds. Primarily, substitutions on the aromatic group and the TZD nitrogen were key areas where activity was enhanced within this group of compounds.

Subject

Animals; Humans; Inbred C57BL; Male; Mice; Models; Molecular; Molecular Structure; Monoamine Oxidase Inhibitors/chemical synthesis/chemistry/*pharmacology; Monoamine Oxidase/*metabolism; Stereoisomerism; Structure-Activity Relationship; Thiazolidinediones/chemical synthesis/chemistry/*pharmacology

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

4798–4803

Issue

16

Volume

21

Citation

Carroll Richard T; Dluzen Dean E; Stinnett Hilary; Awale Prabha S; Funk Max O; Geldenhuys Werner J, “Structure-activity relationship and docking studies of thiazolidinedione-type compounds with monoamine oxidase B.,” NEOMED Bibliography Database, accessed December 7, 2021, https://neomed.omeka.net/items/show/3493.

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