2. Academic Validation
  3. Discovery of GSK1997132B a novel centrally penetrant benzimidazole PPARγ partial agonist

Discovery of GSK1997132B a novel centrally penetrant benzimidazole PPARγ partial agonist

  • Bioorg Med Chem Lett. 2011 Sep 15;21(18):5568-72. doi: 10.1016/j.bmcl.2011.06.088.
Mairi Sime 1,  Amanda C Allan,  Paul Chapman,  Charlotte Fieldhouse,  Gerard M P Giblin,  Mark P Healy,  Millard H Lambert,  Lisa M Leesnitzer,  Ann Lewis,  Raymond V Merrihew,  Richard A Rutter,  Rosemary Sasse,  Barry G Shearer,  Timothy M Willson,  Robert X Xu,  David J Virley
Affiliations

Affiliation

  • 1 Neurosciences Centre for Excellence in Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Harlow, Essex, CM19 5AW, United Kingdom. [email protected]
PMID: 21798739 DOI: 10.1016/j.bmcl.2011.06.088
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.

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