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Aleglitazar, a new, potent, and balanced dual PPAR@a/@c agonist for the treatment of type II diabetes

Agnes Bénardeau, 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, and Peter Mohr

Bioorg Med Chem Lett 19(9):6 (2009) PMID 19349176

Design, synthesis, and SAR of novel @a-alkoxy-@b-arylpropionic acids as potent and balanced PPAR@a@c 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.

DOI: 10.1016/j.bmcl.2009.03.036
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