Aleglitazar, a new, potent, and balanced dual PPARα/γ agonist for the treatment of type II diabetes
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.
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)
Structure-based design of indole propionic acids as novel PPARα/γ co-agonists
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
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)
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