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Discovery of novel and orally active FXR agonists for the potential treatment of dyslipidemia & diabetes |
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| Authors: | Richter Hans G F Benson Gregory M Blum Denise Chaput Evelyne Feng Song Gardes Christophe Grether Uwe Hartman Peter Kuhn Bernd Martin Rainer E Plancher Jean-Marc Rudolph Markus G Schuler Franz Taylor Sven Bleicher Konrad H |
| Affiliation: | a F. Hoffmann-La Roche AG, Grenzacherstrasse, CH-4070 Basel, Switzerland b Roche R&D Center (China) Ltd, 720 Cai Lun Road, Pudong, Shanghai 201203, China |
| Abstract: | Herein we describe the synthesis and structure activity relationship of a new class of FXR agonists identified from a high-throughput screening campaign. Further optimization of the original hits led to molecules that were highly active in an LDL-receptor KO model for dyslipidemia. The most promising candidate is discussed in more detail. |
| Keywords: | Farnesoid X receptor Nuclear hormone receptors Ugi-reaction Benzimidazoles |
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