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Bioorg Med Chem Lett. 2010 Aug 15;20(16):4911-7. doi: 10.1016/j.bmcl.2010.06.084. Epub 2010 Jun 19.

Synthesis and pharmacological validation of a novel series of non-steroidal FXR agonists.

Author information

1
Phenex Pharmaceuticals AG, Waldhofer Strasse 104, 69123 Heidelberg, Germany.

Abstract

To overcome the known liabilities of GW4064 a series of analogs were synthesized where the stilbene double bond is replaced by an oxymethylene or amino-methylene linker connecting a terminal benzoic acid with a substituted heteroaryl in the middle ring position. As a result we discovered compounds with increased potency in vitro that cause dose-dependent reduction of plasma triglycerides and cholesterol in db/db mice down to 2 x 1 mg/kg/day upon oral administration.

PMID:
20638278
DOI:
10.1016/j.bmcl.2010.06.084
[Indexed for MEDLINE]

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