Development of a new class of benzoylpyrrole-based PPARα/γ activators

  • Bioorg Med Chem Lett. 2011 Jan 1;21(1):220-4. doi: 10.1016/j.bmcl.2010.11.032.
Kantaro Ushiroda  1 ,  Katsunori Maruta ,  Makoto Kitoh ,  Kiyotaka Iwai ,  Jun Nagamine ,  Atsushi Tsuchida ,  Mutsuo Taiji ,  Ryu Nagata
Affiliations
  • 1. Dainippon Sumitomo Pharma Co, Ltd, Drug Research Division, Chemistry Research Laboratories, Osaka, Japan.
PMID: 21130649 DOI: 10.1016/j.bmcl.2010.11.032
Abstract

Starting with a subtle blood glucose-lowering effect of a TGF-β inhibitor, we designed and synthesized a series of benzoylpyrrole-based carboxylic acids as PPARs activators. Among these compounds, 10sNa exhibited favorable blood glucose-lowering effect without body weight gain. We assume that the beneficial effect of 10sNa is attributed to not only its compound PPARα agonistic activity but also its PPARγ partial agonistic activity.