Aleglitazar, a new, potent, and balanced dual PPARalpha/gamma agonist for the treatment of type II diabetes

  • Bioorg Med Chem Lett. 2009 May 1;19(9):2468-73. doi: 10.1016/j.bmcl.2009.03.036.
Agnes Bénardeau  1 ,  Jörg Benz ,  Alfred Binggeli ,  Denise Blum ,  Markus Boehringer ,  Uwe Grether ,  Hans Hilpert ,  Bernd Kuhn ,  Hans Peter Märki ,  Markus Meyer ,  Kurt Püntener ,  Susanne Raab ,  Armin Ruf ,  Daniel Schlatter ,  Peter Mohr
Affiliations
  • 1. F. Hoffmann-La Roche Ltd, Pharma Research, CH-4070 Basel, Switzerland.
PMID: 19349176 DOI: 10.1016/j.bmcl.2009.03.036
Abstract

Design, synthesis, and SAR of novel alpha-alkoxy-beta-arylpropionic acids as potent and balanced PPARalphagamma coagonists are described. One representative thereof, Aleglitazar ((S)-2Aa), was chosen for clinical development. Its X-ray structure in complex with both receptors as well as its high efficacy in animal models of T2D and dyslipidemia are also presented.

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