Back to Search Start Over

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

Authors :
Akwabi-Ameyaw A
Caravella JA
Chen L
Creech KL
Deaton DN
Madauss KP
Marr HB
Miller AB
Navas F 3rd
Parks DJ
Spearing PK
Todd D
Williams SP
Wisely GB
Source :
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2011 Oct 15; Vol. 21 (20), pp. 6154-60. Date of Electronic Publication: 2011 Aug 11.
Publication Year :
2011

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.<br /> (Copyright © 2011 Elsevier Ltd. All rights reserved.)

Details

Language :
English
ISSN :
1464-3405
Volume :
21
Issue :
20
Database :
MEDLINE
Journal :
Bioorganic & medicinal chemistry letters
Publication Type :
Academic Journal
Accession number :
21890356
Full Text :
https://doi.org/10.1016/j.bmcl.2011.08.034