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Bioorg Med Chem Lett. 2011 Oct 15;21(20):6154-60. doi: 10.1016/j.bmcl.2011.08.034. Epub 2011 Aug 11.

Conformationally constrained farnesoid X receptor (FXR) agonists: alternative replacements of the stilbene.

Author information

1
Department of Medicinal Chemistry, GlaxoSmithKline, Research Triangle Park, NC 27709, USA.

Abstract

To further explore the optimum placement of the acid moiety in conformationally constrained analogs of GW 4064 1a, a series of stilbene replacements were prepared. The benzothiophene 1f and the indole 1g display the optimal orientation of the carboxylate for enhanced FXR agonist potency.

PMID:
21890356
DOI:
10.1016/j.bmcl.2011.08.034
[Indexed for MEDLINE]

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