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

Bioorganic & Medicinal Chemistry Letters
2009.0

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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