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ID: ALA1138459

Journal: Bioorg Med Chem Lett

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

Authors: Bénardeau A, Benz J, Binggeli A, Blum D, Boehringer M, Grether U, Hilpert H, Kuhn B, Märki HP, Meyer M, Püntener K, Raab S, Ruf A, Schlatter D, Mohr P.

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.

CiteXplore: 19349176

DOI: 10.1016/j.bmcl.2009.03.036