Synthesis and SAR of 2-aryl-3-aminomethylquinolines as agonists of the bile acid receptor TGR5

  • Bioorg Med Chem Lett. 2010 Oct 1;20(19):5718-21. doi: 10.1016/j.bmcl.2010.08.014.
Mark R Herbert  1 ,  Dana L Siegel ,  Lena Staszewski ,  Charmagne Cayanan ,  Urmi Banerjee ,  Sangeeta Dhamija ,  Jennifer Anderson ,  Amy Fan ,  Li Wang ,  Peter Rix ,  Andrew K Shiau ,  Tadimeti S Rao ,  Stewart A Noble ,  Richard A Heyman ,  Eric Bischoff ,  Mausumee Guha ,  Ayman Kabakibi ,  Anthony B Pinkerton
Affiliations
  • 1. Department of Chemistry, Kalypsys, Inc.,10420 Wateridge Circle, San Diego, CA 92121, USA.
PMID: 20801037 DOI: 10.1016/j.bmcl.2010.08.014
Abstract

Optimization of a screening hit from uHTS led to the discovery of TGR5 agonist 32, which was shown to have activity in a rodent model for diabetes.