2. Academic Validation
  3. Synthesis and biological activities of novel indole derivatives as potent and selective PPARgamma modulators

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

Affiliation

  • 1 Department of Medicinal Chemistry, Laboratoire GlaxoSmithKline, Centre de Recherches, 25-27 Avenue du Québec, 91951 Les Ulis, France. yann.lamotte@gsk.com
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.

Figures