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

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. 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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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2010-10, Vol.20 (19), p.5718-5721
Hauptverfasser:	Herbert, Mark R., Siegel, Dana L., Staszewski, Lena, Cayanan, Charmagne, Banerjee, Urmi, Dhamija, Sangeeta, Anderson, Jennifer, Fan, Amy, Wang, Li, Rix, Peter, Shiau, Andrew K., Rao, Tadimeti S., Noble, Stewart A., Heyman, Richard A., Bischoff, Eric, Guha, Mausumee, Kabakibi, Ayman, Pinkerton, Anthony B.
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Bile acids Biological and medical sciences Diabetes Diabetes Mellitus, Type 2 - drug therapy General and cellular metabolism. Vitamins Glucagon-Like Peptide 1 - metabolism GPCRs Hydroxyquinolines - chemical synthesis Hydroxyquinolines - chemistry Hydroxyquinolines - therapeutic use Medical sciences Mice Pharmacology. Drug treatments Quinolines - chemical synthesis Quinolines - chemistry Quinolines - therapeutic use Receptors, G-Protein-Coupled - agonists Receptors, G-Protein-Coupled - metabolism Structure-Activity Relationship TGR5 Thiophenes - chemical synthesis Thiophenes - chemistry Thiophenes - therapeutic use
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Zusammenfassung:	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. 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.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2010.08.014