Synthesis, biological evaluation and molecular investigation of fluorinated peroxisome proliferator-activated receptors alpha/gamma dual agonists (Articolo in rivista)

Type
Label
  • Synthesis, biological evaluation and molecular investigation of fluorinated peroxisome proliferator-activated receptors alpha/gamma dual agonists (Articolo in rivista) (literal)
Anno
  • 2012-01-01T00:00:00+01:00 (literal)
Alternative label
  • Giuseppe Fracchiolla, Antonio Laghezza, Luca Piemontese, Mariagiovanna Parente, Antonio Lavecchia, Giorgio Pochetti, Roberta Montanari, Carmen Di Giovanni, Giuseppe Carbonara, Paolo Tortorella, Ettore Novellino, Fulvio Loiodice (2012)
    Synthesis, biological evaluation and molecular investigation of fluorinated peroxisome proliferator-activated receptors alpha/gamma dual agonists
    in Bioorganic & medicinal chemistry (Print)
    (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#autori
  • Giuseppe Fracchiolla, Antonio Laghezza, Luca Piemontese, Mariagiovanna Parente, Antonio Lavecchia, Giorgio Pochetti, Roberta Montanari, Carmen Di Giovanni, Giuseppe Carbonara, Paolo Tortorella, Ettore Novellino, Fulvio Loiodice (literal)
Pagina inizio
  • 2141 (literal)
Pagina fine
  • 2151 (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#numeroVolume
  • 20 (literal)
Rivista
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#affiliazioni
  • Dipartimento Farmaco-Chimico, Università degli Studi di Bari: G. Fracchiolla, A. Laghezza, L. Piemontese, M. Parente, G. Carbonara, P. Tortorella, F. Loiodice Dipartimento di Chimica Farmaceutica e Tossicologica, 'Drug Discovery' Laboratory, Università di Napoli 'Federico II': A. Lavecchia, C. Di Giovanni E. Novellino Istituto di Cristallografia: Montanari R., Pochetti G. (literal)
Titolo
  • Synthesis, biological evaluation and molecular investigation of fluorinated peroxisome proliferator-activated receptors alpha/gamma dual agonists (literal)
Abstract
  • PPARs are transcription factors that govern lipid and glucose homeostasis and play a central role in cardiovascular decease, 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 PPARalpha and PPARgamma dual agonists. Docking experiments were also carried out to gain insight into the interactions of the most active derivatives with both receptors (literal)
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