Synthesis and biological activities of novel indole derivatives as potent and selective PPARgamma modulators

  • Bioorg Med Chem Lett. 2010 Feb 15;20(4):1399-404. doi: 10.1016/j.bmcl.2009.12.107.
Yann Lamotte  1 ,  Paul Martres ,  Nicolas Faucher ,  Alain Laroze ,  Didier Grillot ,  Nicolas Ancellin ,  Yannick Saintillan ,  Véronique Beneton ,  Robert T Gampe Jr
Affiliations
  • 1. Department of Medicinal Chemistry, Laboratoire GlaxoSmithKline, Centre de Recherches, 25-27 Avenue du Québec, 91951 Les Ulis, France. [email protected]
PMID: 20079636 DOI: 10.1016/j.bmcl.2009.12.107
Abstract

Starting from the structure of Telmisartan, a new series of potent and selective PPARgamma modulators was identified. The synthesis, in vitro and in vivo evaluation of the most potent compounds are reported and the X-ray structure of compound 7b bound to the PPARgamma ligand binding domain is described.