1168138-55-3Relevant academic research and scientific papers
Discovery of GSK1997132B a novel centrally penetrant benzimidazole PPARγ partial agonist
Sime, Mairi,Allan, Amanda C.,Chapman, Paul,Fieldhouse, Charlotte,Giblin, Gerard M.P.,Healy, Mark P.,Lambert, Millard H.,Leesnitzer, Lisa M.,Lewis, Ann,Merrihew, Raymond V.,Rutter, Richard A.,Sasse, Rosemary,Shearer, Barry G.,Wilson, Timothy M.,Xu, Robert X.,Virley, David J.
, p. 5568 - 5572 (2011/10/09)
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.
NOVEL COMPOUNDS
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Page/Page column 34, (2009/08/14)
The invention relates to novel benzimidazole compounds of formula (I) wherein R1 to R1 are as defined in the specification, pharmaceutically acceptable salts thereof, to pharmaceutical compositions containing them and their use in medicine. In particular, the invention relates to compounds that are agonists of peroxisome proliferators-activated receptorγ (PPARγ).
