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Substituted isoxazole analogs of farnesoid X receptor (FXR) agonist GW4064.

Abstract：

:Starting from the known FXR agonist GW 4064 1a, a series of alternately 3,5-substituted isoxazoles was prepared. Several of these analogs were potent full FXR agonists. A subset of this series, with a tether between the isoxazole ring and the 3-position aryl substituent, were equipotent FXR agonists to GW 4064 1a, with the 2,6-dimethyl phenol analog 1t having greater FRET FXR potency than GW 4064 1a.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Bass JY,Caldwell RD,Caravella JA,Chen L,Creech KL,Deaton DN,Madauss KP,Marr HB,McFadyen RB,Miller AB,Parks DJ,Todd D,Williams SP,Wisely GB

doi

10.1016/j.bmcl.2009.04.047

subject

Has Abstract

pub_date

2009-06-01 00:00:00

pages

2969-73

issue

11

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(09)00553-8

journal_volume

19

pub_type

杂志文章

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