2‐Phenoxy‐nicotinamides are Potent Agonists at the Bile Acid Receptor GPBAR1 (TGR5)
ChemMedChem2012Vol. 8(4), pp. 569–576
Citations Over TimeTop 14% of 2012 papers
Rainer E. Martin, Caterina Bissantz, Olivier Gavelle, Christoph Kuratli, Henrietta Dehmlow, Hans Richter, Ulrike Obst Sander, Shawn D. Erickson, Kyung‐Jin Kim, Sherrie Pietranico-Cole, Rubén Alvarez‐Sánchez, Christoph Ullmer
Abstract
Potency with potential: 2-Phenoxy-nicotinamides were identified as potent agonists at the GPBAR1 receptor, a target in the treatment of obesity, type 2 diabetes and metabolic syndrome. Extensive structure-activity relationship studies supported by homology modeling and docking resulted in the identification of optimized GPBAR1 agonists, potent against both human and mouse receptors, endowed with favorable physicochemical properties and good metabolic stability.
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