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Text
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URL Address
<a href="http://doi.org/10.1016/j.bmcl.2011.06.060" target="_blank" rel="noreferrer noopener">http://doi.org/10.1016/j.bmcl.2011.06.060</a>
Pages
4798–4803
Issue
16
Volume
21
Dublin Core
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Title
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Structure-activity relationship and docking studies of thiazolidinedione-type compounds with monoamine oxidase B.
Publisher
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Bioorganic & medicinal chemistry letters
Date
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2011
2011-08
Subject
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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
Creator
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Carroll Richard T; Dluzen Dean E; Stinnett Hilary; Awale Prabha S; Funk Max O; Geldenhuys Werner J
Description
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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.
Identifier
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<a href="http://doi.org/10.1016/j.bmcl.2011.06.060" target="_blank" rel="noreferrer noopener">10.1016/j.bmcl.2011.06.060</a>
Rights
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Article information provided for research and reference use only. All rights are retained by the journal listed under publisher and/or the creator(s).
2011
Animals
Awale Prabha S
Bioorganic & medicinal chemistry letters
Carroll Richard T
Dluzen Dean E
Funk Max O
Geldenhuys Werner J
Humans
Inbred C57BL
Male
Mice
Models
Molecular
Molecular Structure
Monoamine Oxidase Inhibitors/chemical synthesis/chemistry/*pharmacology
Monoamine Oxidase/*metabolism
Stereoisomerism
Stinnett Hilary
Structure-Activity Relationship
Thiazolidinediones/chemical synthesis/chemistry/*pharmacology