Synthesis, biological evaluation and molecular investigation of fluorinated peroxisome proliferator-activated receptors α/γ dual agonists

Bioorganic & Medicinal Chemistry
Giuseppe FracchiollaFulvio Loiodice

Abstract

PPARs are transcription factors that govern lipid and glucose homeostasis and play a central role in cardiovascular disease, obesity, and diabetes. Thus, there is significant interest in developing new agonists for these receptors. Given that the introduction of fluorine generally has a profound effect on the physical and/or biological properties of the target molecule, we synthesized a series of fluorinated analogs of the previously reported compound 2, some of which turned out to be remarkable PPARα and PPARγ dual agonists. Docking experiments were also carried out to gain insight into the interactions of the most active derivatives with both receptors.

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Citations

Oct 7, 2016·Scientific Reports·Davide CapelliAntonio Lavecchia
Aug 31, 2018·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Luca PiemonteseMichele Solfrizzo
Jan 27, 2015·Journal of Computer-aided Molecular Design·Stephanie N LewisDavid R Bevan
Sep 30, 2020·International Journal of Molecular Sciences·Leonardo BrunettiAntonio Laghezza
Apr 3, 2020·Journal of Medicinal Chemistry·Roberta MontanariGiorgio Pochetti

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