Synthesis and biological evaluation of 2-heteroarylthioalkanoic acid analogues of clofibric acid as peroxisome proliferator-activated receptor α agonists

Letizia Giampietro, Alessandra Ammazzalorso, Antonella Giancristofaro, Fabio Lannutti, Giancarlo Bettoni, Barbara De Filippis, Marialuigia Fantacuzzi, Cristina Maccallini, Michele Petruzzelli, Annalisa Morgano, Antonio Moschetta, Rosa Amoroso

Research output: Contribution to journalArticle

19 Citations (Scopus)

Abstract

Aseries of 2-heteroarylthioalkanoic acids were synthesized through systematic structural modifications of clofibric acid and evaluated for human peroxisome proliferator-activated receptor α (PPARα) transactivation activity, with the aim of obtaining new hypolipidemic compounds. Some thiophene and benzothiazole derivatives showing a good activation of the receptor α were screened for activity against the PPARγ isoform. The gene induction of selected compounds was also investigated in the human hepatoma cell line.

Original languageEnglish
Pages (from-to)6224-6232
Number of pages9
JournalJournal of Medicinal Chemistry
Volume52
Issue number20
DOIs
Publication statusPublished - Oct 22 2009

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Clofibric Acid
Peroxisome Proliferator-Activated Receptors
Thiophenes
Acids
Transcriptional Activation
Hepatocellular Carcinoma
Protein Isoforms
Cell Line
Genes

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

Cite this

Giampietro, L., Ammazzalorso, A., Giancristofaro, A., Lannutti, F., Bettoni, G., De Filippis, B., ... Amoroso, R. (2009). Synthesis and biological evaluation of 2-heteroarylthioalkanoic acid analogues of clofibric acid as peroxisome proliferator-activated receptor α agonists. Journal of Medicinal Chemistry, 52(20), 6224-6232. https://doi.org/10.1021/jm900878u

Synthesis and biological evaluation of 2-heteroarylthioalkanoic acid analogues of clofibric acid as peroxisome proliferator-activated receptor α agonists. / Giampietro, Letizia; Ammazzalorso, Alessandra; Giancristofaro, Antonella; Lannutti, Fabio; Bettoni, Giancarlo; De Filippis, Barbara; Fantacuzzi, Marialuigia; Maccallini, Cristina; Petruzzelli, Michele; Morgano, Annalisa; Moschetta, Antonio; Amoroso, Rosa.

In: Journal of Medicinal Chemistry, Vol. 52, No. 20, 22.10.2009, p. 6224-6232.

Research output: Contribution to journalArticle

Giampietro, L, Ammazzalorso, A, Giancristofaro, A, Lannutti, F, Bettoni, G, De Filippis, B, Fantacuzzi, M, Maccallini, C, Petruzzelli, M, Morgano, A, Moschetta, A & Amoroso, R 2009, 'Synthesis and biological evaluation of 2-heteroarylthioalkanoic acid analogues of clofibric acid as peroxisome proliferator-activated receptor α agonists', Journal of Medicinal Chemistry, vol. 52, no. 20, pp. 6224-6232. https://doi.org/10.1021/jm900878u
Giampietro, Letizia ; Ammazzalorso, Alessandra ; Giancristofaro, Antonella ; Lannutti, Fabio ; Bettoni, Giancarlo ; De Filippis, Barbara ; Fantacuzzi, Marialuigia ; Maccallini, Cristina ; Petruzzelli, Michele ; Morgano, Annalisa ; Moschetta, Antonio ; Amoroso, Rosa. / Synthesis and biological evaluation of 2-heteroarylthioalkanoic acid analogues of clofibric acid as peroxisome proliferator-activated receptor α agonists. In: Journal of Medicinal Chemistry. 2009 ; Vol. 52, No. 20. pp. 6224-6232.
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