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  • Title: Structure-based design of indole propionic acids as novel PPARalpha/gamma co-agonists.
    Author: Kuhn B, Hilpert H, Benz J, Binggeli A, Grether U, Humm R, Märki HP, Meyer M, Mohr P.
    Journal: Bioorg Med Chem Lett; 2006 Aug 01; 16(15):4016-20. PubMed ID: 16737814.
    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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