Literature DB >> 21742494

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

Richard T Carroll1, Dean E Dluzen, Hilary Stinnett, Prabha S Awale, Max O Funk, Werner J Geldenhuys.   

Abstract

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 μM). 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.
Copyright © 2011 Elsevier Ltd. All rights reserved.

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Year:  2011        PMID: 21742494     DOI: 10.1016/j.bmcl.2011.06.060

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  5 in total

1.  Binding of thiazolidinediones to the endoplasmic reticulum protein nutrient-deprivation autophagy factor-1.

Authors:  Werner J Geldenhuys; Robert Skolik; Mary E Konkle; Michael A Menze; Timothy E Long; Aaron R Robart
Journal:  Bioorg Med Chem Lett       Date:  2019-02-01       Impact factor: 2.823

2.  Urea/thiourea: efficient, inexpensive and reusable catalysts for the synthesis of pyrazole derivatives with 2-iminothiazolidin-4-one and 2,4-thiazolidinediones under solvent-free conditions.

Authors:  Veera Swamy Konkala; Pramod Kumar Dubey
Journal:  Mol Divers       Date:  2017-01-04       Impact factor: 2.943

3.  Glitazones inhibit human monoamine oxidase but their anti-inflammatory actions are not mediated by VAP-1/semicarbazide-sensitive amine oxidase inhibition.

Authors:  Christian Carpéné; Mathilde Bizou; Karine Tréguer; Mounia Hasnaoui; Sandra Grès
Journal:  J Physiol Biochem       Date:  2015-01-09       Impact factor: 4.158

4.  Synthesis, HIV-1 RT inhibitory, antibacterial, antifungal and binding mode studies of some novel N-substituted 5-benzylidine-2,4-thiazolidinediones.

Authors:  Radhe Shyam Bahare; Swastika Ganguly; Kiattawee Choowongkomon; Supaporn Seetaha
Journal:  Daru       Date:  2015-01-24       Impact factor: 3.117

5.  Ultrasound-assisted synthesis of 2,4-thiazolidinedione and rhodanine derivatives catalyzed by task-specific ionic liquid: [TMG][Lac].

Authors:  Jagir Singh Sandhu
Journal:  Org Med Chem Lett       Date:  2013-03-03
  5 in total

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