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

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 eff...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2009-05, Vol.19 (9), p.2468
Hauptverfasser:	Bénardeau, Agnes, Benz, Jörg, Binggeli, Alfred, Blum, Denise, Boehringer, Markus, Grether, Uwe, Hilpert, Hans, Kuhn, Bernd, Märki, Hans Peter, Meyer, Markus, Püntener, Kurt, Raab, Susanne, Ruf, Armin, Schlatter, Daniel, Mohr, Peter
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Chemistry, Pharmaceutical - methods Crystallography, X-Ray - methods Diabetes Mellitus, Type 2 - drug therapy Drug Design Dyslipidemias - drug therapy Humans Inhibitory Concentration 50 Ligands Models, Chemical Molecular Structure Oxazoles - chemical synthesis Oxazoles - pharmacology PPAR alpha - agonists PPAR gamma - agonists Receptors, Cytoplasmic and Nuclear - metabolism Thiophenes - chemical synthesis Thiophenes - pharmacology
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Zusammenfassung:	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.
ISSN:	1464-3405
DOI:	10.1016/j.bmcl.2009.03.036