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2-Phenoxy-nicotinamides are potent agonists at the bile acid receptor GPBAR1 (TGR5).
- Source :
-
ChemMedChem [ChemMedChem] 2013 Apr; Vol. 8 (4), pp. 569-76. Date of Electronic Publication: 2012 Dec 07. - Publication Year :
- 2013
-
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.<br /> (Copyright © 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.)
Details
- Language :
- English
- ISSN :
- 1860-7187
- Volume :
- 8
- Issue :
- 4
- Database :
- MEDLINE
- Journal :
- ChemMedChem
- Publication Type :
- Academic Journal
- Accession number :
- 23225346
- Full Text :
- https://doi.org/10.1002/cmdc.201200474