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Synthesis and SAR of 2-aryl-3-aminomethylquinolines as agonists of the bile acid receptor TGR5
Authors:Mark R Herbert  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
Institution:1. Department of Chemistry, Kalypsys, Inc.,10420 Wateridge Circle, San Diego, CA 92121, USA;2. Department of Biology, Kalypsys, Inc.,10420 Wateridge Circle, San Diego, CA 92121, USA;3. Department of Pharmacology, Kalypsys, Inc.,10420 Wateridge Circle, San Diego, CA 92121, USA;4. Department of Drug Metabolism and Pharmacokinetics, Kalypsys, Inc.,10420 Wateridge Circle, San Diego, CA 92121, USA
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.
Keywords:
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