475481-90-4Relevant academic research and scientific papers
Aleglitazar, a new, potent, and balanced dual PPARα/γ agonist for the treatment of type II diabetes
Benardeau, Agnes,Benz, Joerg,Binggeli, Alfred,Blum, Denise,Boehringer, Markus,Grether, Uwe,Hilpert, Hans,Kuhn, Bernd,Maerki, Hans Peter,Meyer, Markus,Puentener, Kurt,Raab, Susanne,Ruf, Armin,Schlatter, Daniel,Mohr, Peter
scheme or table, p. 2468 - 2473 (2010/03/24)
Design, synthesis, and SAR of novel α-alkoxy-β-arylpropionic acids as potent and balanced PPARαγ 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.
Structure-based design of indole propionic acids as novel PPARα/γ co-agonists
Kuhn, Bernd,Hilpert, Hans,Benz, Joerg,Binggeli, Alfred,Grether, Uwe,Humm, Roland,Maerki, Hans Peter,Meyer, Markus,Mohr, Peter
, p. 4016 - 4020 (2007/10/03)
In the quest for novel PPARα/γ co-agonists as putative drugs for the treatment of type 2 diabetes and dyslipidemia, we have used a structure-based design approach to identify propionic acids with a 1,5-disubstituted indole scaffold as potent PPARα/γ activ
