2. Academic Validation
  3. Synthesis and biological evaluation of 2-heteroarylthioalkanoic acid analogues of clofibric acid as peroxisome proliferator-activated receptor alpha agonists

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

  • J Med Chem. 2009 Oct 22;52(20):6224-32. doi: 10.1021/jm900878u.
Letizia Giampietro 1,  Alessandra Ammazzalorso,  Antonella Giancristofaro,  Fabio Lannutti,  Giancarlo Bettoni,  Barbara De Filippis,  Marialuigia Fantacuzzi,  Cristina Maccallini,  Michele Petruzzelli,  Annalisa Morgano,  Antonio Moschetta,  Rosa Amoroso
Affiliations

Affiliation

  • 1 Dipartimento di Scienze del Farmaco, Università degli Studi G. d'Annunzio, Chieti, Italy.
PMID: 19791744 DOI: 10.1021/jm900878u
Abstract

A series of 2-heteroarylthioalkanoic acids were synthesized through systematic structural modifications of clofibric acid and evaluated for human Peroxisome Proliferator-activated Receptor alpha (PPARalpha) transactivation activity, with the aim of obtaining new hypolipidemic compounds. Some thiophene and benzothiazole derivatives showing a good activation of the receptor alpha were screened for activity against the PPARgamma isoform. The gene induction of selected compounds was also investigated in the human hepatoma cell line.

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