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Bioorg Med Chem Lett. 2011 Sep 15;21(18):5568-72. doi: 10.1016/j.bmcl.2011.06.088. Epub 2011 Jun 29.

Discovery of GSK1997132B a novel centrally penetrant benzimidazole PPARγ partial agonist.

Author information

  • 1Neurosciences Centre for Excellence in Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Harlow, Essex, CM19 5AW, United Kingdom. m.sime@beatson.gla.ac.uk

Erratum in

  • Bioorg Med Chem Lett. 2013 Feb 15;23(4):1143. Wilson, Timothy M [corrected to Willson, Timothy M].

Abstract

The peroxisome proliferator-activated receptor γ (PPARγ) is a ligand-activated nuclear receptor, thought to play a role in energy metabolism, glucose homeostasis and microglia-mediated neuroinflammation. A novel benzimidazole series of centrally penetrant PPARγ partial agonists has been identified. The optimization of PPARγ activity and in vivo pharmacokinetics leading to the identification of GSK1997132B a potent, metabolically stable and centrally penetrant PPARγ partial agonist, is described.

Copyright © 2011 Elsevier Ltd. All rights reserved.

PMID:
21798739
[PubMed - indexed for MEDLINE]
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