Affiliation: Frankfurt am Main
- Truxillic acid derivatives act as peroxisome proliferator-activated receptor gamma activatorsRamona Steri
Goethe University Frankfurt, Institute of Pharmaceutical Chemistry ZAFES LiFF FIRST, Max von Laue Str 9, 60438 Frankfurt, Germany
Bioorg Med Chem Lett 20:2920-3. 2010..Herein we present the structure-activity relationships of 16 truxillic acid derivatives, investigated by a cell-based reporter gene assay guided by molecular docking analysis...
- SAR studies of acidic dual γ-secretase/PPARγ modulatorsMartina Hieke
Institute of Pharmaceutical Chemistry, Goethe University Frankfurt, Max von Laue Str 9, D 60438 Frankfurt am Main, Germany
Bioorg Med Chem 19:5372-82. 2011..Compound 17 showed an IC(50) Aβ42=2.4 μM and an EC(50) PPARγ=7.2 μM and could be a valuable tool to further evaluate the concept of dual γ-secretase/PPARγ modulators in animal models of Alzheimer's disease...
- Investigation of imatinib and other approved drugs as starting points for antidiabetic drug discovery with FXR modulating activityRamona Steri
Institute of Pharmaceutical Chemistry, ZAFES LiFF Goethe University Frankfurt, Max von Laue Str 9, D 60438 Frankfurt Main, Germany
Biochem Pharmacol 83:1674-81. 2012..We show FXR modulation by selected compounds in a full length FXR transactivation assay and modulation of a FXR target gene by imatinib...
- Rational design of a pirinixic acid derivative that acts as subtype-selective PPARgamma modulatorTheresa M Thieme
Institute of Pharmaceutical Chemistry, ZAFES LiFF FIRST, Goethe University Frankfurt, 60438 Frankfurt, Germany
Bioorg Med Chem Lett 20:2469-73. 2010..Herein we present modifications of pirinixic acid leading to subtype-selective PPARgamma agonists and furthermore the development of a selective PPARgamma modulator guided by molecular docking studies...
- Discovery of a novel class of 2-mercaptohexanoic acid derivatives as highly active PPARalpha agonistsHeiko Zettl
Goethe University Frankfurt, Institute of Pharmaceutical Chemistry ZAFES LiFF, Max von Laue Str 9, D 60348 Frankfurt M, Germany
Bioorg Med Chem Lett 19:4421-6. 2009..Compound 10 represents a low nano molar active PPARalpha activator with excellent selectivity towards PPARgamma...