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

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20 Scopus citations

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 (US)
Pages (from-to)6224-6232
Number of pages9
JournalJournal of Medicinal Chemistry
Volume52
Issue number20
DOIs
StatePublished - Oct 22 2009

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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    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, 52(20), 6224-6232. https://doi.org/10.1021/jm900878u