Author(s): Sime M, Allan AC, Chapman P, Fieldhouse C, Giblin GM,
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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.
This article was published in Bioorg Med Chem Lett
and referenced in Medicinal Chemistry