Structure-based design of indole propionic acids as novel PPARα/γ co-agonists

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2006 Indole derivatives R 0140 Structure-Based Design of Indole Propionic Acids as Novel PPARα/γ Co-Agonists. The indole-based PPAR α/γ co-agonists (I) and (II), which are selective against the 45- 110 δ—isoform, are identified through a scaffold selection process using structure analysis and molecular modeling. Indole propionic acids (II) are submicromolar dual agonists and members of a class of molecules with the opportunity to potentially fine-tune the insulin sensitizing and lipid-lowering effects. — (KUHN*, B.; HILPERT, H.; BENZ, J.; BINGGELI, A.; GRETHER, U.; HUMM, R.; MAERKI, H. P.; MEYER, M.; MOHR, P.; Bioorg. Med. Chem. Lett. 16 (2006) 15, 4016-4020; Res. Dis. Chem., F. Hoffman-La Roche Ltd., CH-4070 Basel, Switz.; Eng.) — H. Hoennerscheid

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