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

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Citation

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

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

Bioorg Med Chem Lett. 2009 Jun 1;19(11):2969-73. doi: 10.1016/j.bmcl.2009.04.047. Epub 2009 Apr 18.

PubMed ID
19410460 [ View in PubMed
]
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.

DrugBank Data that Cites this Article

Polypeptides
NameUniProt ID
Bile acid receptorQ96RI1Details