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

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

Affiliation

  • 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.

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