FXR agonist activity of conformationally constrained analogs of GW 4064 | Health & Environmental Research Online (HERO)

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Citation
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HERO ID

1467905

Reference Type

Journal Article

Title

FXR agonist activity of conformationally constrained analogs of GW 4064

Author(s)

Akwabi-Ameyaw, A; Bass, JY; Caldwell, RD; Caravella, JA; Chen, L; Creech, KL; Deaton, DN; Madauss, KP; Marr, HB; Mcfadyen, RB; Miller, AB; Navas, F; Parks, DJ; Spearing, PK; Todd, D; Williams, SP; Bruce Wisely, G

Year

2009

Is Peer Reviewed?

Yes

Journal

Bioorganic & Medicinal Chemistry Letters
ISSN: 0960-894X
EISSN: 1464-3405

Volume

Issue

Page Numbers

4733-4739

Language

English

PMID

19586769

DOI

10.1016/j.bmcl.2009.06.062

Web of Science Id

WOS:000268358800044

URL

http://://WOS:000268358800044
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Abstract

Two series of conformationally constrained analogs of the FXR agonist GW 4064 1 were prepared. Replacement of the metabolically labile stilbene with either benzothiophene or naphthalene rings led to the identification of potent full agonists 2a and 2g.

Keywords

Farnesoid X receptor; FXR; Nuclear receptor

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