Rational design of a pirinixic acid derivative that acts as subtype-selective PPARgamma modulator.

@article{Thieme2010RationalDO,
  title={Rational design of a pirinixic acid derivative that acts as subtype-selective PPARgamma modulator.},
  author={Theresa M Thieme and Ramona Steri and Ewgenij Proschak and Alexander Paulke and Gisbert Schneider and Manfred Schubert-Zsilavecz},
  journal={Bioorganic & medicinal chemistry letters},
  year={2010},
  volume={20 8},
  pages={2469-73}
}
Peroxisome proliferator-activated receptor gamma (PPARgamma) is involved in glucose and lipid homeostasis. PPARgamma agonists are in clinical use for the treatment of type 2 diabetes. Lately, a new class of selective PPARgamma modulators (SPPARgammaMs) was developed, which are believed to show less side effects than full PPARgamma agonists. We have previously shown that alpha-substitution of pirinixic acid, a moderate agonist of PPARalpha and PPARgamma, leads to low micromolar active balanced… CONTINUE READING