1. Academic Validation
  2. Benzothiazole-based N-(phenylsulfonyl)amides as a novel family of PPARα antagonists

Benzothiazole-based N-(phenylsulfonyl)amides as a novel family of PPARα antagonists

  • Bioorg Med Chem Lett. 2011 Aug 15;21(16):4869-72. doi: 10.1016/j.bmcl.2011.06.028.
Alessandra Ammazzalorso 1 Antonella Giancristofaro Alessandra D'Angelo Barbara De Filippis Marialuigia Fantacuzzi Letizia Giampietro Cristina Maccallini Rosa Amoroso
Affiliations

Affiliation

  • 1 Dipartimento di Scienze del Farmaco, Università degli Studi G. d'Annunzio, Chieti, Italy.
Abstract

The discovery of PPAR antagonists is emerging as an useful tool for elucidating the biological role of the receptor. Here we report the identification of N-(phenylsulfonyl)amides containing the benzothiazole scaffold, a novel class of potent PPARα antagonists obtained from chemical modification of carboxylic acid agonists. In this work, a group of phenylsulfonamides were synthesized and in vitro evaluated against the agonistic effect of GW7647; they showed an inhibitory effect on PPARα activation, with best compounds revealing a dose-dependent antagonistic profile. Some of these antagonists showed also an inhibitory effect on CPT1A pattern expression.

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