Synthesis and SAR of potent LXR agonists containing an indole pharmacophore

  • Bioorg Med Chem Lett. 2009 Feb 15;19(4):1097-100. doi: 10.1016/j.bmcl.2009.01.004.
David G Washburn  1 ,  Tram H Hoang ,  Nino Campobasso ,  Angela Smallwood ,  Derek J Parks ,  Christine L Webb ,  Kelly A Frank ,  Melanie Nord ,  Chaya Duraiswami ,  Christopher Evans ,  Michael Jaye ,  Scott K Thompson
Affiliations
  • 1. Department of Chemistry, Molecular Discovery Research, GlaxoSmithKline Pharmaceuticals, 709 Swedeland Road, King of Prussia, PA 19406, USA. [email protected]
PMID: 19167885 DOI: 10.1016/j.bmcl.2009.01.004
Abstract

A novel series of 1H-indol-1-yl tertiary amine LXR agonists has been designed. Compounds from this series were potent agonists with good rat pharmacokinetic parameters. In addition, the crystal structure of an LXR agonist bound to LXRalpha will be disclosed.