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Bioorg Med Chem Lett. 2011 Jan 1;21(1):191-4. doi: 10.1016/j.bmcl.2010.11.039. Epub 2010 Nov 12.

Discovery of novel and orally active FXR agonists for the potential treatment of dyslipidemia & diabetes.

Author information

1
F Hoffmann-La Roche AG, Grenzacherstrasse, CH-4070 Basel, Switzerland.

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.

PMID:
21134747
DOI:
10.1016/j.bmcl.2010.11.039
[Indexed for MEDLINE]

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