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

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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.

Autore Pugliese

Tutti gli autori

  • LAGHEZZA A.;LOIODICE F.;FRACCHIOLLA G.;CARBONARA G.G.;PIEMONTESE L.;TORTORELLA P.

Titolo volume/Rivista

Non Disponibile

Anno di pubblicazione

2012

ISSN

0968-0896

ISBN

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Numero di citazioni Wos

Nessuna citazione

Ultimo Aggiornamento Citazioni

Non Disponibile

Numero di citazioni Scopus

15

Ultimo Aggiornamento Citazioni

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Settori ERC

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Codici ASJC

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