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. 2006 Aug 1;16(15):4016-20.
doi: 10.1016/j.bmcl.2006.05.007. Epub 2006 Jun 5.

Structure-based design of indole propionic acids as novel PPARalpha/gamma co-agonists

Bernd Kuhn  1 , Hans Hilpert, Jörg Benz, Alfred Binggeli, Uwe Grether, Roland Humm, Hans Peter Märki, Markus Meyer, Peter Mohr
Affiliations

Structure-based design of indole propionic acids as novel PPARalpha/gamma co-agonists

Bernd Kuhn et al. Bioorg Med Chem Lett. .

Abstract

In the quest for novel PPARalpha/gamma 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 PPARalpha/gamma activators. Compounds 13, 24, and 28 are examples of submicromolar dual agonists with different alpha/gamma EC50 ratios that are selective against the delta-isoform. Analysis of the X-ray complex structure of PPARgamma with the indole propionic acid 13 provides a rationalization for some of the observed SAR.

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